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JH-RE-06

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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。

JH-RE-06  纯度: 99.87%

JH-RE-06, 有效的 REV1-REV7 互作抑制剂 (IC50=0.78 μM; Kd=0.42 μM)，靶向与 POLζ 的 REV7 亚基相互作用的 REV1。JH-RE-06 通过阻止诱变 POLζ 的募集来破坏诱变性跨损伤合成 (TLS)。JH-RE-06 可改善化疗效果。

JH-RE-06

JH-RE-06 Chemical Structure

CAS No. : 1361227-90-8

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥7321 In-stock
1 mg ￥3900 In-stock
5 mg ￥7100 In-stock
10 mg ￥12000 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

JH-RE-06 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Kd=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy[1][2].

IC50 & Target

IC50: 0.78 μM (REV1-REV7)[1]
Kd: 0.42 μM (REV1-REV7)[1]
体外研究
(In Vitro)

JH-RE-06 unexpectedly induces dimerization of the REV1 CTD at its REV7-binding surface and blocks the REV1-REV7 interaction[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.
体内研究
(In Vivo)

JH-RE-06 inhibits mutagenic TLS and enhances cisplatin-induced toxicity in cultured human and mouse cell lines[1].
Co-administration of JH-RE-06 with cisplatin suppresses the growth of xenograft human melanomas in mice[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

468.72

Formula

C20H16Cl3N3O4
CAS 号

1361227-90-8
运输条件

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

DMSO : 5 mg/mL (10.67 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1335 mL 10.6673 mL 21.3347 mL
5 mM 0.4267 mL 2.1335 mL 4.2669 mL
10 mM 0.2133 mL 1.0667 mL 2.1335 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。
参考文献

  • [1]. Wojtaszek JL, et al. A Small Molecule Targeting Mutagenic Translesion Synthesis Improves Chemotherapy. Cell. 2019 Jun 27;178(1):152-159.e11.

    [2]. REV1-POLς Inhibition Enhances Cisplatin-Induced Cytotoxicity. Cancer Discov. 2019 Aug;9(8):OF17.

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

菁华JH723可见分光光度计

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菁华JH723可见分光光度计

  • 品牌 菁华|JINGHUA
  • 型号 JH723
  • 商品详情

    性能指标：

    显示器：大屏幕彩色中/英文触摸显示屏

    波长驱动：自动

    波长范围：320~1000nm

    波长准确度：±0.5nm

    波长重复性：0.2nm

    光谱带宽：1.7nm

    透射比准确度：≤0.3%T

    透射比重复：0.1%T

    透射比范围：0~200%T

    吸光度范围：-0.4~4A

    浓度显示范围： 0~99999

    杂散光：≤0.05%T

    稳定性：±0.001A/h

    基线平直度：±0.002A

    噪声：0.0005A

    输出接口：USB RS-232

    扫描功能：高中低

    动力学：具备

     

    功能特性：

    高性能低杂散光1200L/mm光栅，C-T式单色器的结构，进口钨灯，进口光电转换器，确保了仪器具有低杂散光、高分辨率、高光度线性。

    中/英文彩色触摸显示屏，电脑与主机完美融合为一体，使用流畅、方便，一气呵成，清晰直观的显示被测样品的相关数据和图谱。

    自动设置波长，井具有先进的自动修正波长误差功能，使波长准确度更高。

    仪器配有能在Windows操作系统上运行的应用软件，使仪器具有光度、定量、标准曲线等功能，并可海量储存相关数据和图谱曲线。

    大屏幕/触摸屏/人性化操作界面/主机就可以扫描/可直接连接鼠标打印机等外设。

    • 菁华JH754紫外可见分光光度计（停产）

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    菁华JH754紫外可见分光光度计（停产）

  • 品牌 菁华|JINGHUA
  • 型号 JH754
  • 商品详情

    性能指标：
    波长驱动：自动
    波长范围：190~1100nm
    波长准确度：±0.5nm
    波长重复性：0.2nm
    光谱带宽：4nm
    透射比准确度：≤0.3%T
    透射比重复性：0.1%T
    透射比范围：0~200%T
    吸光度范围：-0.4~4A
    浓度显示范围：0~99999
    杂散光：≤0.05%T
    稳定性：±0.001A/h
    噪声：0.0005A 
    输出接口：RS-232
    回归方程：具备
     
    功能特性：
    采用1200L/mm高性能紫外专用光栅，进口长寿命氘灯/钨灯，进口光电转换器，配以先进的C-T单色器结构，使仪器杂散光低、分辨率高、光度线性好。
     宽大的样品室可扩展至10cm样品架，从而拓展了仪器的测试范围。
    自动设置波长，自动调0%T/100%T，T/A的无误差转换。
    具有先进的自动修正波长误差、光源自动切换等功能，保证了仪器的测试精度和连续性。
     仪器具有光度、定量、标准曲线等功能

    • 菁华JH752紫外可见分光光度计（停产）

    发表于由

    菁华JH752紫外可见分光光度计（停产）

  • 品牌 菁华|JINGHUA
  • 型号 JH752
  • 商品详情

    性能指标：
    显示器 大屏幕彩色中/英文触摸显示屏 
    波长驱动 自动 
    波长范围 190nm~1100nm
    波长准确度 ±1nm 
    波长重复性 0.5nm 
    光谱带宽 4nm
    透射比准确度 ≤0.3%T
    透射比重复性 0.1%T
    透射比范围 0~200%T
    吸光度范围 －0.4~4A
    浓度显示范围 0~99999
    杂散光 ≤0.1%T 
    稳定性 ±0.001A/h
    基线平直度 ±0.002A
    噪声 0.0005A
    输出接口 USB RS-232

    功能特性：
    采用1200L/mm高性能紫外专用光栅，进口长寿命氘灯/钨灯，进口光电转换器，配以先进的C-T单色器结构，使仪器杂散光低、分辨率高、光度线性好。
    宽大的样品室可扩展至10cm样品架，从而拓展了仪器的测试范围。
    具有先进的自动修正波长误差、光源自动切换等功能，保证了仪器的测试精度和连续性。
    仪器采用7英寸彩色中/英文触摸显示屏，清晰直观的显示所测样品的各种数据及图谱。
    仪器具有光度、定量、标准曲线等功能。

    • JH-X-119-01

    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。

    JH-X-119-01  纯度: ≥98.0%

    JH-X-119-01 是一种有效的选择性白介素 1 受体相关激酶 1 (IRAK1) 抑制剂。JH-X-119-01 可改善 LPS 诱导的小鼠败血症。JH-X-119-01 抑制 IRAK1，IC50 为 9 nM，而在浓度高达 10 μM 时对 IRAK4 也没有抑制作用。

    JH-X-119-01

    JH-X-119-01 Chemical Structure

    CAS No. : 2227368-54-7

    规格 价格 是否有货 数量
    5 mg ￥1800 In-stock
    10 mg ￥2700 In-stock
    25 mg ￥4900 In-stock
    50 mg ￥7300 In-stock
    100 mg ￥9900 In-stock
    200 mg   询价  
    500 mg   询价  

    * Please select Quantity before adding items.

    JH-X-119-01 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
    • Anti-Infection Compound Library
    • Immunology/Inflammation Compound Library
    • Kinase Inhibitor Library
    • Anti-Cancer Compound Library
    • Anti-Blood Cancer Compound Library

    生物活性

    JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice[1]. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC50 of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM[2].

    IC50 & Target[2]

    IRAK-1

    9 nM (IC50)

    体外研究
    (In Vitro)

    JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation[1]. JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC50 of 57 nM for YSK4[2]. JH-X-119-01 shows moderate cell killing effects in a panel of Waldenström’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC50s ranging from 0.59 to 9.72 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.

    Western Blot Analysis[1]

    Cell Line: RAW 264.7 cells and THP-1 cells
    Concentration: 10 μM
    Incubation Time: 15 minutes
    Result: Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.

    体内研究
    (In Vivo)

    JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg[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.

    Animal Model: C57BL/6 (20-22 g, male) mice[1]
    Dosage: 5 mg/kg and 10 mg/kg
    Administration: Intraperitoneally injected; 5 days
    Result: Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

    分子量

    452.46

    Formula

    C25H20N6O3
    CAS 号

    2227368-54-7
    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 (552.54 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.2101 mL 11.0507 mL 22.1014 mL
    5 mM 0.4420 mL 2.2101 mL 4.4203 mL
    10 mM 0.2210 mL 1.1051 mL 2.2101 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: ≥ 1.98 mg/mL (4.38 mM); Clear solution

      此方案可获得 ≥ 1.98 mg/mL (4.38 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 19.8 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

    *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]. Bin Pan, et al. Selective inhibition of interleukin-1 receptor-associated kinase 1 ameliorates lipopolysaccharide-induced sepsis in mice. Int Immunopharmacol. 2020 Aug;85:106597.

      [2]. John M Hatcher, et al. Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma. ACS Med Chem Lett. 2020 Oct 9;11(11):2238-2243.

    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

    JH-VIII-157-02

    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。

    JH-VIII-157-02  纯度: 99.67%

    JH-VIII-157-02 是 alectinib 的结构类似物，为 ALK 抑制剂，对棘皮动物微管相关蛋白样 4 (EML4)-ALK G1202R 的 IC50 值为 2 nM。

    JH-VIII-157-02

    JH-VIII-157-02 Chemical Structure

    CAS No. : 1639422-97-1

    规格 价格 是否有货 数量
    5 mg ￥5100 In-stock
    10 mg ￥8150 In-stock
    25 mg ￥15500 In-stock
    50 mg   询价  
    100 mg   询价  

    * Please select Quantity before adding items.

    JH-VIII-157-02 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus
    • Kinase Inhibitor Library
    • Protein Tyrosine Kinase Compound Library
    • Anti-Cancer Compound Library
    • CNS-Penetrant Compound Library
    • Anti-Lung Cancer Compound Library
    • Targeted Diversity Library

    生物活性

    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.

    IC50 & Target

    IC50: 2 nM (EML4-ALK G1202R, cell assay), 2 nM (EML4-ALKwt, cell assay), 2 nM (EML4-ALK C1156Y, cell assay), 2 nM (EML4-ALK F1174L, cell assay), 2 nM (EML4-ALK F1174L, cell assay)[1]
    体外研究
    (In Vitro)

    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells. JH-VIII-157-02 also potently inhibits EML4-ALKwt (Eawt), EAC1156Y, EAF1174L, EAS1206Y (IC50, 2 nM), EAG1269A (IC50, 3 nM), EAL1196M (IC50, 58 nM), EA1151Tins (IC50, 107 nM), and EAL1152R (IC50, 196 nM). Moreover, JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4, and the IC50s are 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM respectively. JH-VIII-157-02 exhibits inhibitory growth of cancer cell lines, such as H3122, DFCI76 (L1152R] with EC50s of 5, 19 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.
    体内研究
    (In Vivo)

    JH-VIII-157-02 exhibits good oral bioavailability following an oral dose of 10 mg/kg in mice. JH-VIII-157-02 also penetrates the CNS of mice[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

    465.55

    Formula

    C28H27N5O2
    CAS 号

    1639422-97-1
    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 : ≥ 25 mg/mL (53.70 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 2.1480 mL 10.7400 mL 21.4800 mL
    5 mM 0.4296 mL 2.1480 mL 4.2960 mL
    10 mM 0.2148 mL 1.0740 mL 2.1480 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。
    参考文献

    • [1]. Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308.
    Cell Assay
    [1]

    Cells are seeded at 4000 per well in 96 well plates and exposed to JH-VIII-157-02 in triplicate at 1 nM to 10 μM for 72 hours. Cell viability is evaluated using CellTiter-Glo Luminescent Cell Viability Assay. IC50 values are calculated by nonlinear regression (variable slope) using GraphPad Prism 5 software. Each experiment is repeated for at least twice[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]. Hatcher JM, et al. Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation. J Med Chem. 2015 Dec 10;58(23):9296-9308.

    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

    JH295 hydrate

    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。

    JH295 hydrate  纯度: ≥99.0%

    JH295 hydrate 是一种有效，不可逆和选择性的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 为 770 nM。JH295 hydrate 通过 Cys22 的烷基化抑制细胞 Nek2。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

    JH295 hydrate

    JH295 hydrate Chemical Structure

    规格 价格 是否有货
    1 mg ￥7000 询问价格 & 货期

    * Please select Quantity before adding items.

    JH295 hydrate 的其他形式现货产品:

    JH295

    生物活性

    JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

    IC50 & Target

    IC50: 770 nM (Nek2)[1]
    体外研究
    (In Vitro)

    JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[1].

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

    Western Blot Analysis[1]

    Cell Line: RPMI7951 cells
    Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
    Incubation Time: 45 minutes
    Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.

    分子量

    338.36

    Formula

    C18H18N4O3
    运输条件

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

    • [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.

    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

    JH295 hydrate

    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。

    JH295 hydrate  纯度: ≥99.0%

    JH295 hydrate 是一种有效，不可逆和选择性的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 为 770 nM。JH295 hydrate 通过 Cys22 的烷基化抑制细胞 Nek2。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

    JH295 hydrate

    JH295 hydrate Chemical Structure

    规格 价格 是否有货
    1 mg ￥7000 询问价格 & 货期

    * Please select Quantity before adding items.

    JH295 hydrate 的其他形式现货产品:

    JH295

    生物活性

    JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

    IC50 & Target

    IC50: 770 nM (Nek2)[1]
    体外研究
    (In Vitro)

    JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[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.

    Western Blot Analysis[1]

    Cell Line: RPMI7951 cells
    Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
    Incubation Time: 45 minutes
    Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.

    分子量

    338.36

    Formula

    C18H18N4O3
    运输条件

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

    • [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.

    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

    JH295 hydrate

    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。

    JH295 hydrate  纯度: ≥99.0%

    JH295 hydrate 是一种有效，不可逆和选择性的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 为 770 nM。JH295 hydrate 通过 Cys22 的烷基化抑制细胞 Nek2。JH295 hydrate 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

    JH295 hydrate

    JH295 hydrate Chemical Structure

    规格 价格 是否有货
    1 mg ￥7000 询问价格 & 货期

    * Please select Quantity before adding items.

    JH295 hydrate 的其他形式现货产品:

    JH295

    生物活性

    JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

    IC50 & Target

    IC50: 770 nM (Nek2)[1]
    体外研究
    (In Vitro)

    JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[1].

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

    Western Blot Analysis[1]

    Cell Line: RPMI7951 cells
    Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
    Incubation Time: 45 minutes
    Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.

    分子量

    338.36

    Formula

    C18H18N4O3
    运输条件

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

    • [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.

    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

    北京中惠普解析管活化仪JH-1

    发表于由

    北京中惠普解析管活化仪JH-1

  • 品牌 中惠普|BCHP
  • 型号 JH-1
  • 商品详情

    名称：解析管活化仪 JH-1

    仪器特点：
    1、安装简单，只需将氮气接到仪器进气口即可开机使用
    2、操作简单，程序设置完成后，只需按下运行按钮即可自动运行活化，完成后自动降温
    3、安全可靠，仪器装有安全装置

    技术参数

    温控范围

    控温精度

    室温—380℃
    ± 1℃

    模拟采样流量

    100—1000ml/min

    解析时间

    1分钟至24小时可调

    重复性

    使用电压

    >95%

    220V±10%,50—60Hz

    解析管规格

    Φ6mm 长度>120mm

    • JH-XVII-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。

    JH-XVII-10 

    JH-XVII-10 是一种有效的，具有选择性和口服活性的 DYRK1A 和 DYRK1B 抑制剂，IC50值分别为 3 nM 和 5 nM。JH-XVII-10 在颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XVII-10

    JH-XVII-10 Chemical Structure

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

    * Please select Quantity before adding items.

    生物活性

    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines[1].

    IC50 & Target[1]

    DYRK1A

    3 nM (IC50)

    DYRK1B

    5 nM (IC50)

    体外研究
    (In Vitro)

    JH-XVII-10 (compound 10) (1 µM; CAL27 cells) shows active against JNK1 (IC50=1130 nM), JNK2 (IC50=1100 nM), JNK3 (IC50=>10 000 nM), FAK (IC50=90 nM), RSK1 (IC50=82 nM), RSK2 (IC50=80 nM), RSK3 (IC50=61 nM)[1].
    JH-XVII-10 (10 µM; 72 h) decreases cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively[1].
    JH-XVII-10 (1, 10 µM; 24 h) induces apoptosis in CAL27 cells[1].
    JH-XVII-10 (0.5, 1, 5, 10 µM; 24 h) shows inhibitory effects on pro-tumor signaling in CAL27 cells[1].

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

    Cell Proliferation Assay[1]

    Cell Line: CAL27, FaDu, HEK293FT cells
    Concentration: 10 µM
    Incubation Time: 72 h
    Result: Decreased cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively.

    Western Blot Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 0.5, 1, 5, 10 µM
    Incubation Time: 24 h
    Result: Showed inhibitory effects on pro-tumor signaling.

    Apoptosis Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 1, 10 µM
    Incubation Time: 24 h
    Result: Induced increases in the proapoptotic marker (cleaved PARP), and decreased the expression of antiapoptotic protein BCL-xL.

    体内研究
    (In Vivo)

    JH-XVII-10 (2 mg/kg, i.v.; 10 mg/kg, p.o.) shows oral bioavailability (F=12%)[1]. Pharmacokinetic Parameters of JH-XVII-10 in C57Bl/6 male mice[1].

    administration parameters rat dog
    i.v. T1/2 (h) 1.4±0.3 5.70±1.2
    AUC0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4
    CL (mL/min/kg) 17.6±2.0 149.9±62.5
    Vss (L/kg) 1.7±0.2 828.7±134.2
    p.o. Cmax (ng/mL) 1661.1±916.6 3979.4±483.5
    Tmax(h) 0.9±0.8 1.3±0.5
    T1/2 (h) 1.4±0.2 4.9±0.6
    AUC0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2
    F (%) 54.2 31.8

    C57Bl/6 male mice; 2 mg/kg, i.v.; 10 mg/kg, p.o.[1]

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

    Animal Model: C57Bl/6 male mice[1]
    Dosage:
    Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o.
    Result: Showed oral bioavailability (F=12%).

    分子量

    472.40

    Formula

    C21H16F4N8O
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022; 13(4):577-585.

    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

    JH-XVII-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。

    JH-XVII-10 

    JH-XVII-10 是一种有效的，具有选择性和口服活性的 DYRK1A 和 DYRK1B 抑制剂，IC50值分别为 3 nM 和 5 nM。JH-XVII-10 在颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XVII-10

    JH-XVII-10 Chemical Structure

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

    * Please select Quantity before adding items.

    生物活性

    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines[1].

    IC50 & Target[1]

    DYRK1A

    3 nM (IC50)

    DYRK1B

    5 nM (IC50)

    体外研究
    (In Vitro)

    JH-XVII-10 (compound 10) (1 µM; CAL27 cells) shows active against JNK1 (IC50=1130 nM), JNK2 (IC50=1100 nM), JNK3 (IC50=>10 000 nM), FAK (IC50=90 nM), RSK1 (IC50=82 nM), RSK2 (IC50=80 nM), RSK3 (IC50=61 nM)[1].
    JH-XVII-10 (10 µM; 72 h) decreases cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively[1].
    JH-XVII-10 (1, 10 µM; 24 h) induces apoptosis in CAL27 cells[1].
    JH-XVII-10 (0.5, 1, 5, 10 µM; 24 h) shows inhibitory effects on pro-tumor signaling in CAL27 cells[1].

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

    Cell Proliferation Assay[1]

    Cell Line: CAL27, FaDu, HEK293FT cells
    Concentration: 10 µM
    Incubation Time: 72 h
    Result: Decreased cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively.

    Western Blot Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 0.5, 1, 5, 10 µM
    Incubation Time: 24 h
    Result: Showed inhibitory effects on pro-tumor signaling.

    Apoptosis Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 1, 10 µM
    Incubation Time: 24 h
    Result: Induced increases in the proapoptotic marker (cleaved PARP), and decreased the expression of antiapoptotic protein BCL-xL.

    体内研究
    (In Vivo)

    JH-XVII-10 (2 mg/kg, i.v.; 10 mg/kg, p.o.) shows oral bioavailability (F=12%)[1]. Pharmacokinetic Parameters of JH-XVII-10 in C57Bl/6 male mice[1].

    administration parameters rat dog
    i.v. T1/2 (h) 1.4±0.3 5.70±1.2
    AUC0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4
    CL (mL/min/kg) 17.6±2.0 149.9±62.5
    Vss (L/kg) 1.7±0.2 828.7±134.2
    p.o. Cmax (ng/mL) 1661.1±916.6 3979.4±483.5
    Tmax(h) 0.9±0.8 1.3±0.5
    T1/2 (h) 1.4±0.2 4.9±0.6
    AUC0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2
    F (%) 54.2 31.8

    C57Bl/6 male mice; 2 mg/kg, i.v.; 10 mg/kg, p.o.[1]

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

    Animal Model: C57Bl/6 male mice[1]
    Dosage:
    Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o.
    Result: Showed oral bioavailability (F=12%).

    分子量

    472.40

    Formula

    C21H16F4N8O
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022; 13(4):577-585.

    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

    JH-XVII-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。

    JH-XVII-10 

    JH-XVII-10 是一种有效的，具有选择性和口服活性的 DYRK1A 和 DYRK1B 抑制剂，IC50值分别为 3 nM 和 5 nM。JH-XVII-10 在颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XVII-10

    JH-XVII-10 Chemical Structure

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

    * Please select Quantity before adding items.

    生物活性

    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines[1].

    IC50 & Target[1]

    DYRK1A

    3 nM (IC50)

    DYRK1B

    5 nM (IC50)

    体外研究
    (In Vitro)

    JH-XVII-10 (compound 10) (1 µM; CAL27 cells) shows active against JNK1 (IC50=1130 nM), JNK2 (IC50=1100 nM), JNK3 (IC50=>10 000 nM), FAK (IC50=90 nM), RSK1 (IC50=82 nM), RSK2 (IC50=80 nM), RSK3 (IC50=61 nM)[1].
    JH-XVII-10 (10 µM; 72 h) decreases cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively[1].
    JH-XVII-10 (1, 10 µM; 24 h) induces apoptosis in CAL27 cells[1].
    JH-XVII-10 (0.5, 1, 5, 10 µM; 24 h) shows inhibitory effects on pro-tumor signaling in CAL27 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.

    Cell Proliferation Assay[1]

    Cell Line: CAL27, FaDu, HEK293FT cells
    Concentration: 10 µM
    Incubation Time: 72 h
    Result: Decreased cell proliferation by ~45%, and ~40% for CAL27 and FaDu cells, respectively.

    Western Blot Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 0.5, 1, 5, 10 µM
    Incubation Time: 24 h
    Result: Showed inhibitory effects on pro-tumor signaling.

    Apoptosis Analysis[1]

    Cell Line: CAL27 cells
    Concentration: 1, 10 µM
    Incubation Time: 24 h
    Result: Induced increases in the proapoptotic marker (cleaved PARP), and decreased the expression of antiapoptotic protein BCL-xL.

    体内研究
    (In Vivo)

    JH-XVII-10 (2 mg/kg, i.v.; 10 mg/kg, p.o.) shows oral bioavailability (F=12%)[1]. Pharmacokinetic Parameters of JH-XVII-10 in C57Bl/6 male mice[1].

    administration parameters rat dog
    i.v. T1/2 (h) 1.4±0.3 5.70±1.2
    AUC0-∞ (ng*h/mL) 931.3±95.7 14,830.8±5475.4
    CL (mL/min/kg) 17.6±2.0 149.9±62.5
    Vss (L/kg) 1.7±0.2 828.7±134.2
    p.o. Cmax (ng/mL) 1661.1±916.6 3979.4±483.5
    Tmax(h) 0.9±0.8 1.3±0.5
    T1/2 (h) 1.4±0.2 4.9±0.6
    AUC0-∞ (ng*h/mL) 5044.9±1061 23,109.9±7752.2
    F (%) 54.2 31.8

    C57Bl/6 male mice; 2 mg/kg, i.v.; 10 mg/kg, p.o.[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.

    Animal Model: C57Bl/6 male mice[1]
    Dosage:
    Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o.
    Result: Showed oral bioavailability (F=12%).

    分子量

    472.40

    Formula

    C21H16F4N8O
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022; 13(4):577-585.

    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

    JH-XIV-68-3

    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。

    JH-XIV-68-3 

    JH-XIV-68-3 是 DYRK1A/B 的选择性大环抑制剂。JH-XIV-68-3 在生化和细胞测定中显示出对 DYRK1A 和近亲 DYRK1B 的选择性。JH-XIV-68-3 在头颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XIV-68-3

    JH-XIV-68-3 Chemical Structure

    CAS No. : 2426628-52-4

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

    * Please select Quantity before adding items.

    生物活性

    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines[1].

    分子量

    454.41

    Formula

    C21H17F3N8O
    CAS 号

    2426628-52-4
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022;13(4):577-585.

    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

    JH-XIV-68-3

    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。

    JH-XIV-68-3 

    JH-XIV-68-3 是 DYRK1A/B 的选择性大环抑制剂。JH-XIV-68-3 在生化和细胞测定中显示出对 DYRK1A 和近亲 DYRK1B 的选择性。JH-XIV-68-3 在头颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XIV-68-3

    JH-XIV-68-3 Chemical Structure

    CAS No. : 2426628-52-4

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

    * Please select Quantity before adding items.

    生物活性

    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines[1].

    分子量

    454.41

    Formula

    C21H17F3N8O
    CAS 号

    2426628-52-4
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022;13(4):577-585.

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    JH-XIV-68-3

    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。

    JH-XIV-68-3 

    JH-XIV-68-3 是 DYRK1A/B 的选择性大环抑制剂。JH-XIV-68-3 在生化和细胞测定中显示出对 DYRK1A 和近亲 DYRK1B 的选择性。JH-XIV-68-3 在头颈部鳞状细胞癌 (HNSCC) 细胞系中显示出抗肿瘤功效。

    JH-XIV-68-3

    JH-XIV-68-3 Chemical Structure

    CAS No. : 2426628-52-4

    规格 是否有货
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    生物活性

    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines[1].

    分子量

    454.41

    Formula

    C21H17F3N8O
    CAS 号

    2426628-52-4
    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]. Powell CE, et al. Selective Macrocyclic Inhibitors of DYRK1A/B. ACS Med Chem Lett. 2022;13(4):577-585.

    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

    JH-XVI-178

    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。

    JH-XVI-178 

    JH-XVI-178 是一种高效、选择性的CDK8/19抑制剂，具有低清除率和中等口服药代动力学特性。

    JH-XVI-178

    JH-XVI-178 Chemical Structure

    CAS No. : 2648453-53-4

    规格 是否有货
    100 mg   询价  
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    生物活性

    JH-XVI-178 is a highly potent and selective inhibitor of CDK8/19 that displays low clearance and moderate oral pharmacokinetic properties.

    IC50 & Target

    CDK8

    1 nM (IC50)

    CDK19

    2 nM (IC50)

    分子量

    435.91

    Formula

    C22H22ClN7O
    CAS 号

    2648453-53-4
    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]. Hatcher JM, et al. Development of Highly Potent and Selective Pyrazolopyridine Inhibitor of CDK8/19. ACS Med Chem Lett. 2021 Oct 22;12(11):1689-1693.

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    NVP-BSK805

    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。

    NVP-BSK805 

    NVP-BSK805 是一种 ATP 竞争性的 JAK2 抑制剂，对 JAK2 JH1 (JAK 同源 1)，JAK1 JH1，JAK3 JH1，和 TYK2 JH1 的 IC50 值分别为 0.48 nM，31.63 nM，18.68 nM 和 10.76 nM。

    NVP-BSK805

    NVP-BSK805 Chemical Structure

    CAS No. : 1092499-93-8

    规格 是否有货
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    NVP-BSK805 的其他形式现货产品:

    NVP-BSK805 dihydrochloride

    生物活性

    NVP-BSK805 is an ATP-competitive JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively[1].

    IC50 & Target[1]

    JAK2 JH1

    0.48 nM (IC50)

    FL JAK2 V617F

    0.56 nM (IC50)

    FL JAK2 wt

    0.58 nM (IC50)

    TYK2 JH1

    10.76 nM (IC50)

    JAK3 JH1

    18.68 nM (IC50)

    JAK1 JH1

    31.63 nM (IC50)

    体外研究
    (In Vitro)

    NVP-BSK805 (BSK 805) is a JAK2 inhibitor, with IC50s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC50s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 is ATP-competitive, with aclculated Ki of 0.43 ± 0.02 nM. NVP-BSK805 suppresses the growth of JAK2V617F-bearing acute myeloid leukemia cell lines with GI50 of <100 nm. nvp-bsk805 blocks the stat5 phosphorylation at ≥100 nm concentrations, and shows a bias for jak2 over jak1 jak3 inhibition in jak2V617F-mutant cell lines[1].
    NVP-BSK805 (5 μM) improves P-gp inhibitory activity. NVP-BSK805 increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose[2].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
    体内研究
    (In Vivo)

    NVP-BSK805 (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2V617F cell-driven mouse model[1].
    NVP-BSK805 (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice[1].

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

    490.55

    Formula

    C27H28F2N6O
    CAS 号

    1092499-93-8
    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]. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

      [2]. Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182.
    Cell Assay
    [1]

    The antiproliferative activity of JAK2 inhibitors is determined by incubating cells for 72 hours (96 hours for MB-02 and MUTZ-8 cells) with an 8-point concentration range of NVP-BSK805 and cell proliferation relative to NVP-BSK805 is measured using the colorimetric WST-1 cell viability readout. Of each triplicate treatment, the mean is calculated and these data are plotted in XLfit 4 to determine the half-maximal growth inhibition (GI50) values[1].

    Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Concomitantly with NVP-BSK805 treatment, female BALB/c mice receive daily s.c. injections (in 100 μL saline buffer) of 10 units of rhEpo for 4 consecutive days. Controls are injected corresponding volumes of saline buffer. Mice are sacrificed 24 hours after the final dose and total blood, spleen, and bone marrow are taken for further analysis. Animals are 8 to 10 weeks of age at treatment start (20-25 g body weight) and are kept under optimal hygienic conditions with free access to food and water[1].

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

    • [1]. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

      [2]. Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182.

    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

    JH295

    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。

    JH295  纯度: 99.53%

    JH295 是一种有效，不可逆和选择性的 NIMA-related kinase 2 (Nek2) 抑制剂，IC50 为 770 nM。JH295 通过 Cys22 的烷基化抑制细胞 Nek2。JH295 对有丝分裂激酶 Cdk1，Aurora B 或 Plk1 没有活性，并且不会干扰双极纺锤体组件或纺锤体组件检查点。

    JH295

    JH295 Chemical Structure

    CAS No. : 1311143-71-1

    规格 价格 是否有货 数量
    5 mg ￥4500 In-stock
    10 mg ￥8000 In-stock
    25 mg ￥15500 In-stock
    50 mg ￥23500 In-stock
    100 mg ￥34000 In-stock
    200 mg   询价  
    500 mg   询价  

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    JH295 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus

    生物活性

    JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint[1].

    IC50 & Target

    IC50: 770 nM (Nek2)[1]
    体外研究
    (In Vitro)

    JH295 (Compound 16; 0.08-20 μM; 45 minutes; RPMI7951 cells) treatment inhibits WT Nek2 in cells with an IC50 of ~1.3 μM, whereas it has little effect on the C22V mutant[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.

    Western Blot Analysis[1]

    Cell Line: RPMI7951 cells
    Concentration: 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 6.6 μM, 20 μM
    Incubation Time: 45 minutes
    Result: Inhibited WT Nek2 in cells with an IC50 of ~1.3 μM, whereas had little effect on the C22V mutant.

    分子量

    320.35

    Formula

    C18H16N4O2
    CAS 号

    1311143-71-1
    运输条件

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

    -20°C, stored under nitrogen

    *该产品在溶液状态不稳定，建议您现用现配，即刻使用。
    溶解性数据
    In Vitro: 

    DMSO : 55 mg/mL (171.69 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.1216 mL 15.6079 mL 31.2159 mL
    5 mM 0.6243 mL 3.1216 mL 6.2432 mL
    10 mM 0.3122 mL 1.5608 mL 3.1216 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；该产品在溶液状态不稳定，建议您现用现配，即刻使用。
    参考文献

    • [1]. Jeffrey C Henise, et al. Irreversible Nek2 kinase inhibitors with cellular activity. J Med Chem. 2011 Jun 23;54(12):4133-46.

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    JH-XI-10-02

    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。

    JH-XI-10-02  纯度: 98.18%

    JH-XI-10-02 是由Cereblon配体和CDK配体相连的PROTAC，是一种高效的选择性 PROTAC CDK8 降解剂，IC50 值为 159 nM。JH-XI-10-02 降解 CDK8 蛋白，但对其 mRNA 水平没有影响。JH-XI-10-02 对 CDK19 无作用。

    JH-XI-10-02

    JH-XI-10-02 Chemical Structure

    CAS No. : 2209085-22-1

    规格 价格 是否有货 数量
    1 mg ￥5800 In-stock
    5 mg ￥14500 In-stock
    10 mg ￥23500 In-stock
    25 mg ￥45000 In-stock
    50 mg   询价  
    100 mg   询价  

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    JH-XI-10-02 相关产品

    •相关化合物库:

    • Bioactive Compound Library Plus

    生物活性

    JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1].

    IC50 & Target[1]

    CDK8

    159 nM (IC50)

    Cereblon

     

    体外研究
    (In Vitro)

    JH-XI-10-02, a bivalent small molecule degrader, recruits the E3 ligase CRL4Cereblon to promote the ubiquitination and proteosomal degradation of CDK8[1].
    JH-XI-10-02 (1 μM) induces partial degradation of CDK8 in Jurkat cells upon treatment for 6 h. JH-XI-10-02 (1 μM) induces significant degradation of CDK8 after treatment for 24 h[1].
    JH-XI-10-02 induces degradation of CDK8 at 5 μM in WT Molt4 cells, no degradation in CRBN null Molt4 cells at any concentration (0.1-5 μM) in WT Molt4 cells and Molt4 cells where CRBN had been subject to CRISPER/CAS9-mediated deletion for 24 h[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.

    Western Blot Analysis[1]

    Cell Line: Jurkat cells
    Concentration: 1 μM
    Incubation Time: 6 and 24 hours
    Result: Partial degradation of CDK8 upon treatment for 6 h at a concentration of 1 μM.
    Significant degradation of CDK8 after treatment for 24 h at a concentration of 1 μM.

    Western Blot Analysis[1]

    Cell Line: WT Molt4 and CRBN null Molt4 cells
    Concentration: 0.1, 0.5, 1, 2, 5 μM
    Incubation Time: 24 hours
    Result: Degradation of CDK8 at 5 μM in WT Molt4 cells. There were no degradation in CRBN null Molt4 cells at any concentration.

    分子量

    920.14

    Formula

    C53H69N5O9
    CAS 号

    2209085-22-1
    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 (108.68 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.0868 mL 5.4340 mL 10.8679 mL
    5 mM 0.2174 mL 1.0868 mL 2.1736 mL
    10 mM 0.1087 mL 0.5434 mL 1.0868 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: ≥ 5.75 mg/mL (6.25 mM); Clear solution

      此方案可获得 ≥ 5.75 mg/mL (6.25 mM，饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 57.5 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

    *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]. Hatcher JM, et al. Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8. ACS Med Chem Lett. 2018 Mar 18;9(6):540-545.

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