WDR5-IN-1

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。

WDR5-IN-1  纯度: 98.71%

WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂,Kd 为 <0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT),IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集,并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。

WDR5-IN-1

WDR5-IN-1 Chemical Structure

CAS No. : 2408842-51-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5660 In-stock
5 mg ¥5000 In-stock
10 mg ¥8800 In-stock
50 mg   询价  
100 mg   询价  

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WDR5-IN-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].

体外研究
(In Vitro)

WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1].
WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1]. WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 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.

Cell Cycle Analysis[1]

Cell Line: MV4:11 cells
Concentration: 1 µM
Incubation Time: 48 hours
Result: Showed an approximate 4 fold increased SubG1 cells.

Western Blot Analysis[1]

Cell Line: MV4:11 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM
Incubation Time: 24, 48 hours
Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h.

分子量

514.59

Formula

C30H31FN4O3

CAS 号

2408842-51-1

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 (194.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9433 mL 9.7165 mL 19.4329 mL
5 mM 0.3887 mL 1.9433 mL 3.8866 mL
10 mM 0.1943 mL 0.9716 mL 1.9433 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 (4.86 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.86 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 (4.86 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.86 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
*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]. Tian J, et al.Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core.J Med Chem. 2020 Jan 23;63(2):656-675.

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WDR5-IN-4

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。

WDR5-IN-4 

WDR5-IN-4 是一种染色质相关 WD 重复结构域 5 蛋白 (WDR5) 的 WIN 位点抑制剂,Kd 值为 0.1 nM。WDR5-IN-4 能够从染色质中取代 WDR5,并降低相关基因的表达,引起翻译抑制和核仁应激。具有抗癌作用。

WDR5-IN-4

WDR5-IN-4 Chemical Structure

CAS No. : 2407457-36-5

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WDR5-IN-4 的其他形式现货产品:

WDR5-IN-4 TFA

生物活性

WDR5-IN-4 is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity[1].

IC50 & Target

Kd: 0.1 nM (WIN)[1]

分子量

498.38

Formula

C25H22Cl2FN5O

CAS 号

2407457-36-5

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]. Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13.

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WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

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。

WDR5-0103-d3 (Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) 是 WDR5-0103 的氘代物。WDR5-0103是一个有效的含WD重复序列蛋白5 (WDR5) 选择性拮抗剂, Kd 值为450 nM。

WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 Chemical Structure

CAS No. : 2733719-50-9

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

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) is the deuterium labeled WDR5-0103. WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.

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. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

分子量

386.46

Formula

C21H22D3N3O4

CAS 号

2733719-50-9

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

    [2]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.

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

WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

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。

WDR5-0103-d3 (Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) 是 WDR5-0103 的氘代物。WDR5-0103是一个有效的含WD重复序列蛋白5 (WDR5) 选择性拮抗剂, Kd 值为450 nM。

WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 Chemical Structure

CAS No. : 2733719-50-9

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

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) is the deuterium labeled WDR5-0103. WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.

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. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

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

分子量

386.46

Formula

C21H22D3N3O4

CAS 号

2733719-50-9

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

    [2]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.

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

WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

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。

WDR5-0103-d3 (Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) 是 WDR5-0103 的氘代物。WDR5-0103是一个有效的含WD重复序列蛋白5 (WDR5) 选择性拮抗剂, Kd 值为450 nM。

WDR5-0103-d3(Synonyms: WD-Repeat Protein 5-0103-d3)

WDR5-0103-d3 Chemical Structure

CAS No. : 2733719-50-9

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

WDR5-0103-d3 (WD-Repeat Protein 5-0103-d3) is the deuterium labeled WDR5-0103. WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.

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. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[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

386.46

Formula

C21H22D3N3O4

CAS 号

2733719-50-9

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

    [2]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[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: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 cells[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: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

MS33

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。

MS33 

MS33 是一种有效的 WDR5 降解剂,对 VCBWDR5Kd 值分别为 870 nM 和 120 nM。MS33 以 E3 连接酶 VHL 和蛋白酶体依赖性方式诱导 WDR5 降解。MS33 可用于急性髓系白血病的研究。

MS33

MS33 Chemical Structure

CAS No. : 2407449-11-8

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

MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia[1][2][3].

IC50 & Target[1]

VHL

 

WDR5

120 nM (Kd)

VCB

870 nM (Kd)

体外研究
(In Vitro)

MS33 (0.05-5 μM; 18 h) induces WDR5 degradation in a concentration-dependent manner in MV4;11 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.

Western Blot Analysis[1]

Cell Line: MV4;11 cells
Concentration: 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 1, 2, 4, 8, 16, 24 hours
Result: Concentration- and time-dependently induced WDR5 degradation.
The DC50 of MS33 was 260 nM, and the maximum degradation of 71%.

分子量

1208.48

Formula

C64H84F3N11O7S

CAS 号

2407449-11-8

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]. Yu X, et, al. A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models. Sci Transl Med. 2021 Sep 29;13(613):eabj1578.

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

MM-401

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。

MM-401 

MM-401 有效抑制 MLL1-WDR5 相互作用,IC50 为 0.9 nM。 MM-401 对 WDR5 具有高结合亲和力 (Ki<1 nM)。 MM-401 特异性抑制 MLL1 H3 赖氨酸 (K) 4 甲基转移酶活性,但不影响其他 MLL 家族组蛋白甲基转移酶 (HMT)。 MM-401可用于MLL白血病的研究。

MM-401

MM-401 Chemical Structure

CAS No. : 1442106-10-6

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

MM-401 is a potent inhibitor for the MLL1-WDR5 interaction with the IC50 of 0.9 nM in disrupting WDR5-MLL1 interaction. MM-401 maintains high binding affinity to WDR5 (Ki<1 nm). mm-401 specifically inhibits mll1 h3 lysine (k) 4 methyltransferase activity but does not affect other mll family histone methyltransferases (hmts). can be used for the research of leukemia[1].

分子量

586.73

Formula

C29H46N8O5

CAS 号

1442106-10-6

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]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.

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MM-401

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。

MM-401 

MM-401 有效抑制 MLL1-WDR5 相互作用,IC50 为 0.9 nM。 MM-401 对 WDR5 具有高结合亲和力 (Ki<1 nM)。 MM-401 特异性抑制 MLL1 H3 赖氨酸 (K) 4 甲基转移酶活性,但不影响其他 MLL 家族组蛋白甲基转移酶 (HMT)。 MM-401可用于MLL白血病的研究。

MM-401

MM-401 Chemical Structure

CAS No. : 1442106-10-6

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

MM-401 is a potent inhibitor for the MLL1-WDR5 interaction with the IC50 of 0.9 nM in disrupting WDR5-MLL1 interaction. MM-401 maintains high binding affinity to WDR5 (Ki<1 nm). mm-401 specifically inhibits mll1 h3 lysine (k) 4 methyltransferase activity but does not affect other mll family histone methyltransferases (hmts). can be used for the research of leukemia[1].

分子量

586.73

Formula

C29H46N8O5

CAS 号

1442106-10-6

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]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.

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

MM-401

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。

MM-401 

MM-401 有效抑制 MLL1-WDR5 相互作用,IC50 为 0.9 nM。 MM-401 对 WDR5 具有高结合亲和力 (Ki<1 nM)。 MM-401 特异性抑制 MLL1 H3 赖氨酸 (K) 4 甲基转移酶活性,但不影响其他 MLL 家族组蛋白甲基转移酶 (HMT)。 MM-401可用于MLL白血病的研究。

MM-401

MM-401 Chemical Structure

CAS No. : 1442106-10-6

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

MM-401 is a potent inhibitor for the MLL1-WDR5 interaction with the IC50 of 0.9 nM in disrupting WDR5-MLL1 interaction. MM-401 maintains high binding affinity to WDR5 (Ki<1 nm). mm-401 specifically inhibits mll1 h3 lysine (k) 4 methyltransferase activity but does not affect other mll family histone methyltransferases (hmts). can be used for the research of leukemia[1].

分子量

586.73

Formula

C29H46N8O5

CAS 号

1442106-10-6

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]. Fang Cao, et al. Targeting MLL1 H3K4 methyltransferase activity in mixed-lineage leukemia. Mol Cell. 2014 Jan 23;53(2):247-61.

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WDR5-0103(Synonyms: WD-Repeat Protein 5-0103)

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。

WDR5-0103 (Synonyms: WD-Repeat Protein 5-0103) 纯度: 98.11%

WDR5-0103是一个有效的含WD重复序列蛋白5 (WDR5) 选择性拮抗剂, Kd值为450 nM。

WDR5-0103(Synonyms: WD-Repeat Protein 5-0103)

WDR5-0103 Chemical Structure

CAS No. : 890190-22-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥792 In-stock
5 mg ¥720 In-stock
10 mg ¥1200 In-stock
50 mg ¥5000 In-stock
100 mg ¥8000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

WDR5-0103 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM. IC50 value: 450 nM (Kd) Target: WDR5 in vitro: WDR5-0103 inhibits MLL catalytic activity with an IC50 value of 39±10 μM. An increase in MLL complex concentration resulted in proportional increase in IC50 values for WDR5-0103 (83±10 and 280±12 μM at concentrations of 500 and 1000 nM of the core trimeric MLL complex respectively). These data are consistent with a mechanism of action in which WDR5-0103 antagonizes the interaction of WDR5 with MLL by competing with MLL for their mutual binding site on WDR5.

分子量

383.44

Formula

C21H25N3O4

CAS 号

890190-22-4

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 : 50 mg/mL (130.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6080 mL 13.0399 mL 26.0797 mL
5 mM 0.5216 mL 2.6080 mL 5.2159 mL
10 mM 0.2608 mL 1.3040 mL 2.6080 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 (6.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.52 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 (6.52 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.52 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 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 (6.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.52 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]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159.

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WDR5-IN-4 TFA

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。

WDR5-IN-4 TFA  纯度: 98.43%

WDR5-IN-4 TFA 是一种染色质相关 WD 重复结构域 5 蛋白 (WDR5) 的 WIN 位点抑制剂,Kd 值为 0.1 nM。WDR5-IN-4 TFA 能够从染色质中取代 WDR5,并降低相关基因的表达,引起翻译抑制和核仁应激。具有抗癌作用。

WDR5-IN-4 TFA

WDR5-IN-4 TFA Chemical Structure

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4720 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
50 mg ¥16500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

WDR5-IN-4 TFA 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Histone Modification Research Compound Library
  • Anti-Cancer Compound Library
  • Reprogramming Compound Library
  • Anti-Blood Cancer Compound Library

生物活性

WDR5-IN-4 TFA is an inhibitor of the WIN site of chromatin-associated WD repeat-containing protein 5 (WDR5), with a Kd of 0.1 nM. WDR5-IN-4 TFA displaces WDR5 from chromatin and decreases the expression of associated genes, causing translational inhibition, nucleolar stress. Anti-cancer activity[1].

分子量

612.40

Formula

C27H23Cl2F4N5O3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 250 mg/mL (408.23 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 1.6329 mL 8.1646 mL 16.3292 mL
5 mM 0.3266 mL 1.6329 mL 3.2658 mL
10 mM 0.1633 mL 0.8165 mL 1.6329 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 (stored under nitrogen, away from moisture)。-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]. Aho ER, et al. Displacement of WDR5 from Chromatin by a WIN Site Inhibitor with Picomolar Affinity. Cell Rep. 2019 Mar 12;26(11):2916-2928.e13.

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