1. PROTAC Metabolic Enzyme/Protease
  2. PROTACs E1/E2/E3 Enzyme
  3. CRBN-6-5-5-VHL

CRBN-6-5-5-VHL 是一种有效的选择性的基于 von Hippel-Lindau E3 配体的 cereblon (CRBN) 降解剂,DC50 值为 1.5 nM。CRBN-6-5-5-VHL 对底物 IKZF1IKZF3 的降解几乎没有影响。(粉色:VHL 配体 (HY-125845),蓝色:E3 连接酶配体 (HY-10984);黑色:连接子 (HY-403544))。

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CRBN-6-5-5-VHL Chemical Structure

CRBN-6-5-5-VHL Chemical Structure

CAS No. : 2362575-45-7

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544))[1].

IC50 & Target[1]

Cereblon

1.5 nM (DC50)

体外研究
(In Vitro)

CRBN-6-5-5-VHL (0.001-10 μM,24 小时) 可诱导 MM1S 细胞中 CRBN 降解,在 1 μM 时诱导其完全降解[1]
CRBN-6-5-5-VHL (100 nM,96 小时) 通过阻止诱导 IKZF1IKZF3 降解来保护或拯救 MM1S 细胞免受免疫调节亚胺类药物 (IMiD) 毒性[1]
CRBN-6-5-5-VHL (100 nM,24 小时) 在MM1S 细胞中降解 CRBN 依赖于由 VHL (E3 连接酶)、异质 PROTAC (降解剂) 和 CRBN (靶标) 组成的必需异质三元复合物[1]
CRBN-6-5-5-VHL (100 nM,4-72 小时) 在 MM1S 细胞中使 CRBN 水平低于 50% 持续超过 48 小时,表明具有可持续作用[1]

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

Cell Viability Assay[1]

Cell Line: MM1S
Concentration: 100 nM
Incubation Time: 96 h
Result: Protect or rescue MM1S cells from IMiD toxicity by preventing induction of IKZF1 and IKZF3 degradation.

Western Blot Analysis[1]

Cell Line: MM1S
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 24 h
Result: No reduction of the VHL protein level was observed, however, CRBN levels were decreased.
Showed a negligible effect on the degradation of the neo-substrates IKZF1 and IKZF3.
Treatment with 1 µM for 24 hours induced complete degradation of CRBN, whereas for up to 10 µM no changes in the VHL protein levels were observed.

Western Blot Analysis[1]

Cell Line: MM1S
Concentration: 100 nM
Incubation Time: 24 h
Result: Co-treatment of an excess of Pomalidomide (HY-10984) (POM) caused an impaired capability for CRBN degradation.
Co-treatment with VH298 (HY-100947) abrogated CRBN degradation and depleted IKZF1 and IKZF3.
Genetic VHL knockdown prevented CRBN degradation.

Western Blot Analysis[1]

Cell Line: MM1S
Concentration: 100 nM
Incubation Time: 4, 8, 24, 48, 72 h
Result: Had sustainable effects on MM1S cells, as CRBN levels below 50% were maintained for more than 48 h.
分子量

972.20

Formula

C51H69N7O10S

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 113.33 mg/mL (116.57 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0286 mL 5.1430 mL 10.2859 mL
5 mM 0.2057 mL 1.0286 mL 2.0572 mL
查看完整储备液配制表

* 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 (sealed storage, 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.45%

参考文献

完整储备液配制表

* 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 (sealed storage, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0286 mL 5.1430 mL 10.2859 mL 25.7149 mL
5 mM 0.2057 mL 1.0286 mL 2.0572 mL 5.1430 mL
10 mM 0.1029 mL 0.5143 mL 1.0286 mL 2.5715 mL
15 mM 0.0686 mL 0.3429 mL 0.6857 mL 1.7143 mL
20 mM 0.0514 mL 0.2571 mL 0.5143 mL 1.2857 mL
25 mM 0.0411 mL 0.2057 mL 0.4114 mL 1.0286 mL
30 mM 0.0343 mL 0.1714 mL 0.3429 mL 0.8572 mL
40 mM 0.0257 mL 0.1286 mL 0.2571 mL 0.6429 mL
50 mM 0.0206 mL 0.1029 mL 0.2057 mL 0.5143 mL
60 mM 0.0171 mL 0.0857 mL 0.1714 mL 0.4286 mL
80 mM 0.0129 mL 0.0643 mL 0.1286 mL 0.3214 mL
100 mM 0.0103 mL 0.0514 mL 0.1029 mL 0.2571 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
CRBN-6-5-5-VHL
目录号:
HY-136262
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