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  4. PROTAC HMGCR Degrader-2

PROTAC HMGCR Degrader-2 是一种靶向 HMGCR 的 PROTAC 降解剂，其 IC50 为 0.25 μM。PROTAC HMGCR Degrader-2 可在 Insig 基因沉默的人肝癌细胞 (HepG2) 中降解 HMGCR，DC50 为 0.12 μM。PROTAC HMGCR Degrader-2 的口服前药是 PROTAC HMGCR Degrader-1 (HY-171823)。PROTAC HMGCR Degrader-2 可通过缺氧诱导因子脯氨酰羟化酶 (VHL) 依赖的泛素-蛋白酶体系统降解 HMGCR，并降低人肝癌细胞 (HepG2) 内的胆固醇水平。PROTAC HMGCR Degrader-2 可用于高血脂症相关研究。
(粉色: HMG-CoA Reductase (HMGCR) 配体 (HY-122439)；蓝色: VHL 配体 (HY-125845)；黑色: 连接子 (HY-W014831))。

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PROTAC HMGCR Degrader-2

PROTAC HMGCR Degrader-2 Chemical Structure

CAS No. : 2715104-46-2

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PROTAC HMGCR Degrader-2 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research[1]. (Pink: HMG-CoA Reductase (HMGCR) ligand (HY-122439); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

IC50 & Target[1]

VHL

 

体外研究
(In Vitro)

PROTAC HMGCR Degrader-2 (compound 21c) (0.01-3 μmol/L，16 小时) 在人肝癌细胞 (HepG2) 中，高剂量时更倾向于发挥 HMGCR 抑制剂的作用而非降解剂作用，在 1 μM 的高剂量下，其最大降解率 (Dmax) 可达 65%[1]。
PROTAC HMGCR Degrader-2 (0.1 μM，24 小时) 可降低人肝癌细胞 (HepG2) 内的胆固醇水平[1]。
PROTAC HMGCR Degrader-2 (0.01-3 μM，0-48 小时) 可在 Insig 基因沉默的人肝癌细胞 (HepG2) 中通过 PROTAC 机制介导 HMGCR 降解，其 DC50 为 0.12 μM，在 1 μM 浓度下 Dmax 可达 76%[1]。
PROTAC HMGCR Degrader-2 (1 μM，作用 6 小时) 可在 Insig 基因沉默的人肝癌细胞 (HepG2) 中同时结合 HMGCR 与 VHL，进而通过 VHL 依赖的泛素-蛋白酶体系统降解 HMGCR[1]。

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

PROTAC HMGCR Degrader-2 相关抗体:

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 16 h
Result: Attenuated the upregulation of HMGCR at low doses and increased HMGCR expression at high doses.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.01 μM
Incubation Time: 24 h
Result: Reduced cellular cholesterol protein expression.

Western Blot Analysis[1]

Cell Line: Insig-silenced HepG2 cells
Concentration: 0.01, 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 0, 4, 8, 16, 24 and 48 h
Result: Effectively degraded the HMGCR protein at a dose manner concentration and 16 h.
Elevated HMGCR expression at higher concentration of 3 μM.
Reduced HMGCR protein level in a time-dependent manner at 1 μM.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 1 μM
Incubation Time: 16 h
Result: Effectively attenuated the compensatory upregulation of HMGCR.

Western Blot Analysis[1]

Cell Line: Insig-silenced HepG2 cells
Concentration: 1 μM
Incubation Time: 16 h
Result: Induced HMGCR degradation, which was significantly blocked by the addition of VHL032 (10 μM) or MG132 (10 μM) (HY-13259).
Induced HMGCR degradation reduced by lovastatin (HY-N0504).
分子量

978.29

Formula

C53H79N5O10S
CAS 号
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.
纯度 & 产品资料
参考文献

PROTAC HMGCR Degrader-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

PROTAC HMGCR Degrader-22715104-46-2PROTAC HMGCR Degrader2PROTAC HMGCR Degrader 2PROTACsliver cancerHMGCRPROTACVHLInhibitorinhibitorinhibit

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