标签归档：cdk

多肽定制CDK5 Substrate [PK-pT-PKKAKKL], Phosphoryl 编码

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名称 CDK5 Substrate [PK-pT-PKKAKKL], Phosphoryl
编码
别名 CDK5 Substrate [PK-pT-PKKAKKL], Phosphoryl
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） PK-pT-PKKAKKL
序列（三字母缩写） H-Pro-Lys-pThr-Pro-Lys-Lys-Ala-Lys-Lys-Leu-OH (trifluoroacetate salt)
基本描述 The native peptide PKTPKKAKKL is derived from histone H1 peptide sequence that is docked in the active site of cyclin-dependent kinase 5. It is an effective CDK5 substrate (Km = 40 碌M).
溶解度
分子量 1218.5
化学式
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents CDK5 Substrate [PK-pT-PKKAKKL], Phosphoryl 编码
Figures CDK5 Substrate [PK-pT-PKKAKKL], Phosphoryl 编码
Reference Lew, J. Biochem. 42, 849 (2003) Sharma, P. et al. J. Biol. Chem. 274, 9600 (1999)
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化学桥

多肽定制CDK5 Substrate [PKTPKKAKKL] 编码

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名称 CDK5 Substrate [PKTPKKAKKL]
编码
别名 CDK5 Substrate [PKTPKKAKKL]
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） PKTPKKAKKL
序列（三字母缩写） H-Pro-Lys-Thr-Pro-Lys-Lys-Ala-Lys-Lys-Leu-OH (trifluoroacetate salt)
基本描述 The native peptide PKTPKKAKKL is derived from histone H1 peptide sequence that is docked in the active site of cyclin-dependent kinase 5. It is an effective CDK5 substrate (Km = 40 碌M).
溶解度
分子量 1138.45
化学式 C53H99N15O12
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents CDK5 Substrate [PKTPKKAKKL] 编码
Figures CDK5 Substrate [PKTPKKAKKL] 编码
Reference Lew, J. Biochem. 42, 849 (2003) Sharma, P. et al. J. Biol. Chem. 274, 9600 (1999)
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化学桥

多肽定制CDK5 Substrate [PKTPKKAKKL], Biotinylated 编码

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名称 CDK5 Substrate [PKTPKKAKKL], Biotinylated
编码
别名 CDK5 Substrate [PKTPKKAKKL], Biotinylated
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） Biotin-PKTPKKAKKL
序列（三字母缩写） Biotin-Pro-Lys-Thr-Pro-Lys-Lys-Ala-Lys-Lys-Leu-OH (trifluoroacetate salt)
基本描述 This dibenzylated derivative was found to completely inhibit HIV-1-induced cell fusion and infection in vitro
溶解度
分子量 1364.75
化学式 C63H113N17O14S1
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents CDK5 Substrate [PKTPKKAKKL], Biotinylated 编码
Figures CDK5 Substrate [PKTPKKAKKL], Biotinylated 编码
Reference Lew, J. Biochem. 42, 849 (2003) Sharma, P. et al. J. Biol. Chem. 274, 9600 (1999)
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化学桥

CDK-IN-2(Synonyms: CDK inhibitor II)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK-IN-2 (Synonyms: CDK inhibitor II) 纯度: 98.82%

CDK-IN-2是CDK特异性抑制剂，IC50值为<8 nM。

CDK-IN-2(Synonyms: CDK inhibitor II)

CDK-IN-2 Chemical Structure

CAS No. : 1269815-17-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1761 In-stock
2 mg ￥1100 In-stock
5 mg ￥2200 In-stock
10 mg ￥3200 In-stock
50 mg ￥9900 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CDK-IN-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM, extracted from reference 1, example 4. IC50 Value: <8 nM [1] Target: CDK9 In vitro: In vivo:

IC50 & Target[1]

CDK9/cyclinT1

8 nM (IC50)

分子量

363.81

Formula

C18H19ClFN3O2
CAS 号

1269815-17-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (274.87 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7487 mL 13.7434 mL 27.4869 mL
5 mM 0.5497 mL 2.7487 mL 5.4974 mL
10 mM 0.2749 mL 1.3743 mL 2.7487 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.25 mg/mL (8.93 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.93 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3.25 mg/mL (8.93 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.93 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 3.25 mg/mL (8.93 mM); Clear solution

    此方案可获得 ≥ 3.25 mg/mL (8.93 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 32.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Keith B Pfister, et al. Heteroaryl compounds as kinase inhibitors. 2011, WO2011026917A1.

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HDAC1/2 and CDK2-IN-1

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

HDAC1/2 and CDK2-IN-1 

HDAC1/2 and CDK2-IN-1 (compound 14d) 是一种有效的 HDAC1，HDAC2 和 CDK2 抑制剂，IC50 分别为 70.7，23.1 和 0.80 μM。HDAC1/2 and CDK2-IN-1 可阻断细胞周期，诱导细胞凋亡 (apoptosis)。HDAC1/2 and CDK2-IN-1 表现出良好的体内抗肿瘤活性。

HDAC1/2 and CDK2-IN-1

HDAC1/2 and CDK2-IN-1 Chemical Structure

CAS No. : 2418559-01-8

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生物活性

HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity[1].

IC50 & Target[1]

HDAC1

70.7 nM (IC50)

HDAC2

23.1 nM (IC50)

CDK2

0.80 nM (IC50)

体外研究
(In Vitro)

HDAC1/2 and CDK2-IN-1 (compound 14d) shows excellent antiproliferative activities against H460, A375, HepG2, HCT116 and Hela cells with IC50 values of 1.59, 0.47, 0.86, 0.58 and 1.05 μM, respectively[1].
HDAC1/2 and CDK2-IN-1 (0.5 μM, 48 h) significantly inhibits the migration of H460 and A375 cells[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 24 h) significantly blocks the cell cycle in the G2/M phase[1].
HDAC1/2 and CDK2-IN-1 (0-2 μM, 48 h) promotes cancer cell apoptosis in a dose-dependent manner[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 12 h) inhibits CDK2 and HDAC activity, causing cancer cell death[1].
HDAC1/2 and CDK2-IN-1 (1 μM, 24 h) strongly increases ROS levels in A375 cells, causes cancer cell death by improving intracellular ROS levels[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis

Cell Line: A375, HCT116, H460 and Hela cells[1]
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Significantly blocked the cell cycle, induced a loss of G0/G1 phase cells and an increase of G2/M phase cells, led to an apparent accumulation of cells in G2/M phase at 0.5 μM (A375, the percentage from 13.70 to 57.03%; HCT116, from 27.46 to 76.99%; Hela, from 7.89% to 51.85%).

Apoptosis Analysis

Cell Line: A375, HCT116, H460 and Hela cell lines[1]
Concentration: 0, 0.5, 1, 2 μM
Incubation Time: 48 h
Result: Promoted cancer cell apoptosis in a dose-dependent manner, with the apoptosis rates of 91.99% (A375), 89.60% (HCT116), 59.10% (H460), and 22.36% (Hela) respectively at the concentration of 2 μM.

Immunofluorescence

Cell Line: A375 cells[1]
Concentration: 1 μM
Incubation Time: 12 h
Result: Significantly inhibited CDK2 and increased the acetylation level of histone H3, inhibited CDK2 and HDAC activity, causing cancer cell death.

体内研究
(In Vivo)

HDAC1/2 and CDK2-IN-1 (BALB/c nude mice, 0-100 mg/kg, IP, once daily for 21 days) significantly inhibits the tumor growth[1].
HDAC1/2 and CDK2-IN-1 (compound 14d) (ICR mice; 4 mg/kg, IV; 20 mg/kg, IP) exhibits desirable pharmacokinetic properties[1].
Pharmacokinetic Parameters of HDAC1/2 and CDK2-IN-1 in male ICR mice[1].

Dose (mg/kg) 4 20
Administration IV IP
T1/2 (h) 1.48 2.84
Tmax (h) 2
Cmax (ng/mL) 1360
AUC0-t (ng/mL*h) 2850 7240
MRT0-t (h) 0.563 4.54
CL (mL/(min/kg)) 23.3
F (%) 50.8

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (n = 9)[1]
Dosage: 4 mg/kg (IV), 20 mg/kg (IP)
Administration: IV, IP, once (Pharmacokinetic Analysis)
Result: Exhibited desirable pharmacokinetic properties.
Animal Model: BALB/c nude mice (5-6 weeks, HCT116 xenograft model)[1]
Dosage: 0, 25, 50 and 100 mg/kg
Administration: IP, once daily for 21 days
Result: Significantly inhibited the tumor growth, the tumor growth inhibitions were 28%, 40% and 44% at doses of 25, 50 and 100 mg/kg, respectively.

分子量

483.95

Formula

C26H22ClN7O
CAS 号

2418559-01-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Yun F, Cheng C, Ullah S, Yuan Q. Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer. Eur J Med Chem. 2020;198:112322.

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CDK12-IN-3

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CDK12-IN-3  纯度: 98.22%

CDK12-IN-3 是一种有效，选择性的 CDK12 抑制剂，酶试验中 IC50 值为 491 nM。

CDK12-IN-3

CDK12-IN-3 Chemical Structure

CAS No. : 2220184-50-7

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥4658 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
25 mg ￥15000 In-stock
50 mg ￥25500 In-stock
100 mg ￥43500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CDK12-IN-3 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC50 of 491 nM in enzymatic assay.

IC50 & Target[1]

CDK12

491 nM (IC50)

体外研究
(In Vitro)

CDK12-IN-3 is a highly selective CDK12 inhibitor profiled across a panel of 352 kinases at 0.1 µM. CDK12-IN-3 shows potent inhibition of phosphorylation of Ser2 on the CTD repeat domain of RNA Pol II as well as growth inhibition of OV90 cells and acute cytotoxicity to THP1 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

470.52

Formula

C23H28F2N8O
CAS 号

2220184-50-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (531.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1253 mL 10.6265 mL 21.2531 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 mL
10 mM 0.2125 mL 1.0627 mL 2.1253 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

    此方案可获得 ≥ 2.33 mg/mL (4.95 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

    此方案可获得 ≥ 2.33 mg/mL (4.95 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 23.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Johannes JW, et al. Structure-Based Design of Selective Noncovalent CDK12 Inhibitors. ChemMedChem. 2018 Feb 6;13(3):231-235.

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PROTAC CDK9 degrader-2

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

PROTAC CDK9 degrader-2 

PROTAC CDK9 degrader-2 是一种基于 PROTAC 技术，高效选择性的 CDK9 降解剂，在 MCF-7 细胞系中抑制 CDK9 的 IC50 值为 17 μM。PROTAC 由天然产物汉黄芩素 (Wogonin，CDK配体) 与Cereblon泛素 E3 连接酶 (CRBN) 通过 linker 连接而成。

PROTAC CDK9 degrader-2

PROTAC CDK9 degrader-2 Chemical Structure

CAS No. : 2435721-30-3

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250 mg   询价  
500 mg   询价  

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生物活性

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC[1].

IC50 & Target[1]

CDK9

17 μM (IC50, MCF-7 cells)

分子量

748.74

Formula

C39H36N6O10
CAS 号

2435721-30-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

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生物活性分子抑制剂CVT-313(Synonyms: Cdk2 Inhibitor III)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CVT-313 (Synonyms: Cdk2 Inhibitor III) 纯度: 99.45%

CVT-313 (Cdk2 Inhibitor III) 是一种有效的ATP-竞争性的选择性 CDK2 抑制剂，IC50 为 0.5 μM。CVT-313 可抑制 CDC5L 磷酸化。

CVT-313(Synonyms: Cdk2 Inhibitor III)

CVT-313 Chemical Structure

CAS No. : 199986-75-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥900 In-stock
5 mg ￥818 In-stock
10 mg ￥1228 In-stock
50 mg ￥4297 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CVT-313 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation[1].

IC50 & Target[1]

cdk2/cyclin A

0.5 μM (IC50)

Cdk1/cyclin B

4.2 μM (IC50)

Cdk4/cyclin D1

215 μM (IC50)

体外研究
(In Vitro)

CVT-313 (Cdk2 Inhibitor III) has been shown to inhibit other kinases, but at much higher IC50 values, i.e., CDK1 (IC50=4.2 μM), CDK4 D1 (IC50=215 μM), and MAPK/PKA/PKC (IC50>1.25 mM), compared to CDK2 (IC50=0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM[1]. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC50 of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (Ki=95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity. Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC50 for growth inhibition ranged from 1.25 to 20 μM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

400.47

Formula

C20H28N6O3
CAS 号

199986-75-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (249.71 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4971 mL 12.4853 mL 24.9707 mL
5 mM 0.4994 mL 2.4971 mL 4.9941 mL
10 mM 0.2497 mL 1.2485 mL 2.4971 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803.

    [2]. Brooks EE, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.
Kinase Assay
[1]

For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100 μL 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM NaVO3 and the specific inhibitor at 30°C for 10 minutes. Cell extract as a source of kinase activity is prepared from subconfluent, serum-stimulated COS-7 cells lysed in 20 mM HEPES-NaOH, pH 7.5, 50 mM NaCl, 1% Triton X-100, 10% glycerol, protease and phosphotase inhibitors. Phosphorylated proteins are separated by electrophoresis in 15% polyacrylamide-SDS gels. Specific inhibitors included 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS and 50 μM PD98059[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

MRC-5 cells are grown in Dulbecco’s modified Eagle’s medium containing 5% fetal calf serum. CVT313 (0, 5, 10, 15 μM) is added to exponentially growing cells in tissue culture. Cell population is measured. Proliferation assays are carried out using the nonradioactive CellTiter 96 kit after 48-h exposure. For FACS analysis of DNA content, cells are trypsinized, fixed in 70% ice-cold ethanol, and treated with 0.1 mg/mL RNase A and 40 μg/mL propidium iodide for 1 h at 37°C[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803.

    [2]. Brooks EE, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

生物活性分子抑制剂CVT-313(Synonyms: Cdk2 Inhibitor III)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。
CVT-313 (Synonyms: Cdk2 Inhibitor III) 纯度: 99.45%

CVT-313 (Cdk2 Inhibitor III) 是一种有效的ATP-竞争性的选择性 CDK2 抑制剂，IC50 为 0.5 μM。CVT-313 可抑制 CDC5L 磷酸化。

CVT-313(Synonyms: Cdk2 Inhibitor III)

CVT-313 Chemical Structure

CAS No. : 199986-75-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥900 In-stock
5 mg ￥818 In-stock
10 mg ￥1228 In-stock
50 mg ￥4297 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CVT-313 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation[1].

IC50 & Target[1]

cdk2/cyclin A

0.5 μM (IC50)

Cdk1/cyclin B

4.2 μM (IC50)

Cdk4/cyclin D1

215 μM (IC50)

体外研究
(In Vitro)

CVT-313 (Cdk2 Inhibitor III) has been shown to inhibit other kinases, but at much higher IC50 values, i.e., CDK1 (IC50=4.2 μM), CDK4 D1 (IC50=215 μM), and MAPK/PKA/PKC (IC50>1.25 mM), compared to CDK2 (IC50=0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM[1]. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC50 of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (Ki=95 nM), and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity. Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC50 for growth inhibition ranged from 1.25 to 20 μM[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

400.47

Formula

C20H28N6O3
CAS 号

199986-75-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (249.71 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4971 mL 12.4853 mL 24.9707 mL
5 mM 0.4994 mL 2.4971 mL 4.9941 mL
10 mM 0.2497 mL 1.2485 mL 2.4971 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.24 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.24 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803.

    [2]. Brooks EE, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.
Kinase Assay
[1]

For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100 μL 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM NaVO3 and the specific inhibitor at 30°C for 10 minutes. Cell extract as a source of kinase activity is prepared from subconfluent, serum-stimulated COS-7 cells lysed in 20 mM HEPES-NaOH, pH 7.5, 50 mM NaCl, 1% Triton X-100, 10% glycerol, protease and phosphotase inhibitors. Phosphorylated proteins are separated by electrophoresis in 15% polyacrylamide-SDS gels. Specific inhibitors included 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS and 50 μM PD98059[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

MRC-5 cells are grown in Dulbecco’s modified Eagle’s medium containing 5% fetal calf serum. CVT313 (0, 5, 10, 15 μM) is added to exponentially growing cells in tissue culture. Cell population is measured. Proliferation assays are carried out using the nonradioactive CellTiter 96 kit after 48-h exposure. For FACS analysis of DNA content, cells are trypsinized, fixed in 70% ice-cold ethanol, and treated with 0.1 mg/mL RNase A and 40 μg/mL propidium iodide for 1 h at 37°C[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803.

    [2]. Brooks EE, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CDK4-IN-1-d6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK4-IN-1-d6 

CDK4-IN-1-d6 是一种 CDK4-IN-1 氘代物。CDK4-IN-1 (compound 63) 是一种 CDK4 抑制剂 (IC50= 10 nM)。

CDK4-IN-1-d6

CDK4-IN-1-d6 Chemical Structure

规格 价格 是否有货
1 mg ￥4500 询问价格 & 货期
5 mg ￥12500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

CDK4-IN-1-d6 is a deuterium labeled CDK4-IN-1. CDK4-IN-1 (compound 63) is a CDK4 inhibitor (IC50= 10 nM)[1].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

447.01

Formula

C22H23D6ClN8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Cho YS, Borland M, Brain C, et al. 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. J Med Chem. 2010;53(22):7938-7957.

    [2]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

YKL-5-124

发表于由

YKL-5-124  纯度: 98.03%

YKL-5-124 是一种有效的、选择性不可逆 CDK7 共价抑制剂，对 CDK7 和 CDK7/Mat1/CycH 的 IC50 分别为 53.5 nM 和 9.7 nM。YKL-5-124 对 CDK7 的选择性比 CDK9 和 CDK2 高 100 倍以上，并且对 CDK12 和 CDK13 没有活性。YKL-5-124 诱导强烈的细胞周期停滞，并抑制 E2F 驱动的基因表达，并且对 RNA 聚合酶 II 磷酸化状态几乎没有影响。

YKL-5-124

YKL-5-124 Chemical Structure

CAS No. : 1957203-01-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2890 In-stock
5 mg ￥2550 In-stock
10 mg ￥4350 In-stock
25 mg ￥6960 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

YKL-5-124 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Covalent Screening Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status[1].

IC50 & Target[1]

CDK7

53.5 nM (IC50)

CDK7/Mat1/CycH

9.7 nM (IC50)

CDK2

1300 nM (IC50)

CDK9

3020 nM (IC50)

体外研究
(In Vitro)

YKL-5-124 (0-2000 nM; 72 hours; HAP1 cells) treatment causes a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells[1].
YKL-5-124 (0-2000 nM; 24 hours; HAP1 WT cells) treatment inhibits CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion[1].
Treatment of cells with YKL-5-124 as a competitor at a concentration of about 30 nM blocks pull-down of CDK7-cyclin H but has no effect on the pull-down of cyclin K-CDK12/13 in HAP1 cells. Treatment with 100 nM YKL-5-124 reduces CDK7-cyclin H binding to bioTHZ1 by >50% at 30 min[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis[1]

Cell Line: HAP1 cells
Concentration: 0 nM, 0.2 nM, 0.7 nM, 2 nM, 6.3 nM, 20 nM, 60 nM, 200 nM, 633.3 nM, 2000 nM
Incubation Time: 72 hours
Result: Caused a dose-dependent increase in G1- and G2/M-phase cells and a corresponding loss of S-phase cells.

Western Blot Analysis[1]

Cell Line: HAP1 cells
Concentration: 0 nM, 125 nM, 250 nM, 500 nM, 1000 nM, 2000 nM
Incubation Time: 24 hours
Result: Inhibited CDK1 T-loop phosphorylation, and to a lesser extent CDK2 T-loop phosphorylation in a concentration-dependent fashion.

分子量

515.61

Formula

C28H33N7O3
CAS 号

1957203-01-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (193.95 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9395 mL 9.6973 mL 19.3945 mL
5 mM 0.3879 mL 1.9395 mL 3.8789 mL
10 mM 0.1939 mL 0.9697 mL 1.9395 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.03 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (4.03 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [1]. Olson CM, et al. Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype. Cell Chem Biol. 2019 Jun 20;26(6):792-803.e10.

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CDK7-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK7-IN-1  纯度: 98.91%

CDK7-IN-1，是YKL-5-124 的类似物，是一种细胞周期蛋白依赖性激酶 7 (cdk7) 抑制剂，IC50 值小于 100 nM，来自专利 WO 2016105528 A2 化合物实例 215。

CDK7-IN-1

CDK7-IN-1 Chemical Structure

CAS No. : 1957203-02-9

规格 价格 是否有货 数量
1 mg ￥1900 In-stock
5 mg ￥5900 询价
10 mg ￥9900 询价
25 mg ￥19900 询价
50 mg ￥29900 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

生物活性

CDK7-IN-1, an analog of YKL-5-124, is a cyclin-dependent kinase 7 (cdk7) inhibitor, with an IC50 of less than 100 nM, extracted from patent WO 2016105528 A2, Compound 215[1].

IC50 & Target[1]

CDK7

100 nM (IC50)

分子量

517.62

Formula

C28H35N7O3
CAS 号

1957203-02-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Nathanael S. Gray, et al Inhibitors of cyclin-dependent kinase 7 (cdk7). WO 2016105528 A2

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CDK9-IN-8

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK9-IN-8  纯度: 99.06%

CDK9-IN-8是高效，选择性的 CDK9 抑制剂，IC50为12 nM。

CDK9-IN-8

CDK9-IN-8 Chemical Structure

CAS No. : 2105956-51-0

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥5500 In-stock
50 mg ￥16500 In-stock
100 mg ￥22500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CDK9-IN-8 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

CDK9-IN-8 is a highly effective and selective CDK9 inhibitor with an IC50 of 12 nM.

IC50 & Target[1]

CDK9

12 nM (IC50)

分子量

569.63

Formula

C31H32FN7O3
CAS 号

2105956-51-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5.2 mg/mL (9.13 mM; ultrasonic and warming and heat to 80°C)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7555 mL 8.7776 mL 17.5553 mL
5 mM 0.3511 mL 1.7555 mL 3.5111 mL
10 mM — — —

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Li Y, et al. Discovery of a highly potent, selective and novel CDK9 inhibitor as an anticancer drug candidate. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3231-3237.

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CDK9-IN-7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK9-IN-7  纯度: 99.81%

CDK9-IN-7 (compound 21e) 是一种高效选择性的，具有口服活性的 CDK9/cyclin T 抑制剂 (IC50=11 nM)，与抑制其他 CDK 相比更有效 (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM)。CDK9-IN-7 具有抗癌活性并没有明显的毒性。CDK9-IN-7 诱导非小细胞肺癌 (NSCLC) 细胞凋亡，在 G2 期阻滞细胞周期，并具有抑制非小细胞肺癌干细胞特性。

CDK9-IN-7

CDK9-IN-7 Chemical Structure

CAS No. : 2369981-71-3

规格 价格 是否有货 数量
5 mg ￥6300 In-stock
10 mg ￥9800 In-stock
50 mg ￥28000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CDK9-IN-7 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Orally Active Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Lung Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

CDK9-IN-7 (compound 21e) is a selective, highly potent, and orally active CDK9/cyclin T inhibitor (IC50=11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD=148 nM; CDK6/cyclinD=145 nM). CDK9-IN-7 shows antitumor activity without obvious toxicity. CDK9-IN-7 induces NSCLC cell apoptosis, arrests the cell cycle in the G2 phase, and suppresses the stemness properties of NSCLC[1].

IC50 & Target[1]

CDK9/cyclinT1

11 nM (IC50)

CDK4/cyclin D

148 nM (IC50)

CDK6/cyclinD

145 nM (IC50)

体外研究
(In Vitro)

CDK9-IN-7 displays exceptional potency against NSCLC cell lines, especial A549 and H1299 with IC50 values less than 0.5 µM. In the drug-resistant NSCLC cell line H1975, CDK9-IN-7 also exhibits good inhibition potency with an IC50 value of 0.837 µM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

547.71

Formula

C29H37N7O2S
CAS 号

2369981-71-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (114.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8258 mL 9.1289 mL 18.2578 mL
5 mM 0.3652 mL 1.8258 mL 3.6516 mL
10 mM 0.1826 mL 0.9129 mL 1.8258 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.80 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.80 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.80 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Wang X, et al. Novel cyclin-dependent kinase 9 (CDK9) inhibitor with suppression of cancer stemness activity against non-small-cell lung cancer. Eur J Med Chem. 2019 Jul 25;181:111535.

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CDK12-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK12-IN-2  纯度: 99.44%

CDK12-IN-2是一种高效、选择性的纳摩尔级别的CDK12 抑制剂 (IC50=52 nM)，具有良好的物理化学性质。CDK12-IN-2也是一种强的CDK13抑制剂，因为CDK13是CDK12最接近的同源物。CDK12-IN-2对CDK12的激酶选择性比CDK2、9、8和7高。CDK12-IN-2抑制RNA polymerase II 的 C端Ser2磷酸化。CDK12-IN-2可以作为一种很好的化学探针用于CDK12的功能研究。

CDK12-IN-2

CDK12-IN-2 Chemical Structure

CAS No. : 2244987-03-7

规格 价格 是否有货 数量
5 mg ￥3500 In-stock
10 mg ￥6000 In-stock
25 mg ￥11500 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

CDK12-IN-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

CDK12-IN-2 is a potent, selective and nanomolar CDK12 inhibitor (IC50=52 nM) with good physicochemical properties. CDK12-IN-2 is also a strong CDK13 inhibitor due to CDK13 is the closest homologue of CDK12. CDK12-IN-2 shows excellent kinase selectivity for CDK12 over CDK2, 9, 8, and 7. CDK12-IN-2 inhibits the phosphorylation of Ser2 in the C-terminal domain of RNA polymerase II. CDK12-IN-2 can be used an excellent chemical probe for functional studies of CDK12[1].

IC50 & Target[1]

CDK12

52 nM (IC50)

CDK2

>100 μM (IC50)

CDK7

>10 μM (IC50)

CDK9

16 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-2 inhibits the phosphorylation of the CTD Ser2 in SK-BR-3 cells at low submicromolar concentrations, it inhibits C-terminal domain ser2 phosphorylation with an IC50 of 185 nM. And CDK12-IN-2 exhibits a growth inhibition with an IC50 of 0.8 μM in SK-BR-3 cells[1].
CDK12-IN-2 exhibits time dependency for CDK12 inhibition, the IC50 value for CDK12-IN-2 are 0.0078 μM, 0.042 μM, 0.057 μM,and 0.059 μM, for 0h, 1h, 2h and 5h respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

532.64

Formula

C32H32N6O2
CAS 号

2244987-03-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Masahiro Ito, et al. Discovery of 3-Benzyl-1-( trans-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-arylurea Derivatives as Novel and Selective Cyclin-Dependent Kinase 12 (CDK12) Inhibitors. J Med Chem. 2018 Sep 13;61(17):7710-7728.

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CDK4/6-IN-2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK4/6-IN-2  纯度: 99.82%

CDK4/6-IN-2 是一种有效的 CDK4 和 CDK6 抑制剂，IC50 分别为 2.7 和 16 nM，详细信息请参考专利文献 US20180000819A1 中 的化合物 1。

CDK4/6-IN-2

CDK4/6-IN-2 Chemical Structure

CAS No. : 1800506-48-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3232 In-stock
5 mg ￥2900 In-stock
10 mg ￥4600 In-stock
50 mg ￥13900 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CDK4/6-IN-2 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Cell Cycle/DNA Damage Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Anti-Breast Cancer Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

CDK4/6-IN-2 is a potent CDK4 and CDK6 inhibitor extracted from patent US20180000819A1, Compound 1, has IC50s of 2.7 and 16 nM for CDK4 and CDK6, respectively[1].

IC50 & Target[1]

CDK4

2.7 nM (IC50)

CDK6

16 nM (IC50)

体外研究
(In Vitro)

CDK4/6-IN-2 inhibits H358, H441, PC3, MV-4-11, JeKo-1, SW780, and HGC-27 cells with IC50s of 290.9, 147.8, 260.5, 139, 36.98, 162.5, and 316.4 nM, respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

506.59

Formula

C27H32F2N8
CAS 号

1800506-48-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5.2 mg/mL (10.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9740 mL 9.8699 mL 19.7398 mL
5 mM 0.3948 mL 1.9740 mL 3.9480 mL
10 mM 0.1974 mL 0.9870 mL 1.9740 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.52 mg/mL (1.03 mM); Clear solution

    此方案可获得 ≥ 0.52 mg/mL (1.03 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.2 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.52 mg/mL (1.03 mM); Clear solution

    此方案可获得 ≥ 0.52 mg/mL (1.03 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 5.2 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 0.52 mg/mL (1.03 mM); Clear solution

    此方案可获得 ≥ 0.52 mg/mL (1.03 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 5.2 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Frank Wu, et al. Kinase inhibitor and use thereof. US20180000819A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CDK9-IN-11

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK9-IN-11 

CDK9-IN-11 是一种有效的 CDK9 抑制剂。CDK9-IN-11 是 PROTAC CDK9 Degrader-1 (HY-103628) 的配体。

CDK9-IN-11

CDK9-IN-11 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

CDK9-IN-11 is a potent CDK9 inhibitor. CDK9-IN-11 is the ligand for the PROTAC CDK9 Degrader-1 (HY-103628)[1].

IC50 & Target[1]

CDK9

 

分子量

371.43

Formula

C20H25N3O4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Robb CM, et al. Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC). Chem Commun (Camb). 2017 Jul 4;53(54):7577-7580.

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CDK9-IN-10

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK9-IN-10 

CDK9-IN-10 是一种有效的 CDK9 抑制剂。CDK9-IN-10 是 PROTAC CDK9 degrader-2 (HY-112811) 的配体。

CDK9-IN-10

CDK9-IN-10 Chemical Structure

CAS No. : 3542-63-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

CDK9-IN-10 is a potent CDK9 inhibitor. CDK9-IN-10 is the ligand for the PROTAC CDK9 degrader-2 (HY-112811)[1].

IC50 & Target[1]

CDK9

 

分子量

360.36

Formula

C22H16O5
CAS 号

3542-63-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Bian J, et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

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GSK-3/CDK5/CDK2-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK-3/CDK5/CDK2-IN-1  纯度: 98.56%

GSK-3/CDK5/CDK2-IN-1，一种咪唑衍生物，是 cdk5，cdk2 和 GSK-3 的抑制剂。GSK-3/CDK5/CDK2-IN-1 可用于癌症和神经退行性疾病的研究。详细信息请参考专利文献 WO2002010141A1 中的化合物 9a。

GSK-3/CDK5/CDK2-IN-1

GSK-3/CDK5/CDK2-IN-1 Chemical Structure

CAS No. : 395074-72-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3850 In-stock
5 mg ￥3500 In-stock
10 mg ￥5800 In-stock
25 mg ￥11000 In-stock
50 mg   询价  
100 mg   询价  

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GSK-3/CDK5/CDK2-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
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生物活性

GSK-3/CDK5/CDK2-IN-1, an imidazole derivative, is an inhibitor of cdk5, cdk2, and GSK-3 extracted from patent WO2002010141A1, example 9a. GSK-3/CDK5/CDK2-IN-1 can be used for the research of cancer, and neurodegenerative diseases[1].

IC50 & Target

cdk5[1]
cdk2[1]
GSK-3[1]
体外研究
(In Vitro)

GSK-3/CDK5/CDK2-IN-1 inhibits the phosphorylation of cdk5 peptide substrate phosphorylation, with an IC50 of less than about 50 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

362.42

Formula

C21H22N4O2
CAS 号

395074-72-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (275.92 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7592 mL 13.7961 mL 27.5923 mL
5 mM 0.5518 mL 2.7592 mL 5.5185 mL
10 mM 0.2759 mL 1.3796 mL 2.7592 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Ahlijanian MK, et, al. Preparation of acylaminoimidazoles as inhibitors of cdk5, cdk2, and GSK-3. WO2002010141A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CDK8-IN-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CDK8-IN-1 

CDK8-IN-1 是一个有效的、CDK8 的选择性抑制剂，其 IC50 值为 3 nM。

CDK8-IN-1

CDK8-IN-1 Chemical Structure

CAS No. : 1629633-48-2

规格 价格 是否有货
5 mg ￥3500 询问价格 & 货期
10 mg ￥5500 询问价格 & 货期
25 mg ￥9900 询问价格 & 货期
50 mg ￥16500 询问价格 & 货期
100 mg ￥22500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

CDK8-IN-1 is a potent and selective CDK8 inhibitor with an IC50 of 3 nM.

IC50 & Target[1]

CDK8

3 nM (IC50)

体内研究
(In Vivo)

CDK8-IN-1 displays low systemic clearance, very good exposure and oral bioavailability. The tmax is 0.25 h by PO. The mean values of Cmax are 9940 μg/L, 12740 μg/L by IV and PO respectively. The values of AUC are 9378, 25952 by IV and PO respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

255.20

Formula

C11H8F3N3O
CAS 号

1629633-48-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Han X, et al. Discovery of potent and selective CDK8 inhibitors through FBDD approach. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4488-4492.
Animal Administration
[1]

Mice[1]
CDK8-IN-1 is administrated to mice with 5 mg/kg, 25mg/mg by IV and PO respectively[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [1]. Han X, et al. Discovery of potent and selective CDK8 inhibitors through FBDD approach. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4488-4492.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务