1. PROTAC Metabolic Enzyme/Protease
  2. PROTACs Carbonic Anhydrase
  3. PROTAC hCAII degrader-1

PROTAC hCAII degrader-1 是一种强效的 PROTAC 人碳酸酐酶 II (hCAII) 降解剂,在 HEK293 细胞中的 DC50 为 0.5 nM。PROTAC hCAII degrader-1 可募集 cereblon (CRBN) E3 泛素连接酶以形成三元复合物。PROTAC hCAII degrader-1 可介导 hCAII 的泛素化及随后的蛋白酶体降解
(粉色: CA Ⅱ 配体 (HY-B0989);蓝色: Cereblon 配体 (HY-41547);黑色: 连接子)。

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PROTAC hCAII degrader-1

PROTAC hCAII degrader-1 Chemical Structure

CAS No. : 2892306-56-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII[1]. (Pink: CA Ⅱ ligand (HY-B0989); Blue: Cereblon ligand (HY-41547); Black: linker).

IC50 & Target[1]

hCA II

0.5 nM (DC50)

体外研究
(In Vitro)

PROTAC hCAII degrader-1 (化合物 Degrader 11)(5 pM-15 μM;0-48 h) 可在 HEK293 细胞中强效降解 hCAII,其 DC50 为 0.5 nM,Dₘₐₓ 为 100%,且活性可维持 48 小时以上[1]
PROTAC hCAII degrader-1 (50 nM;6 h) 在 HEK293 细胞中与 Lenalidomide (HY-A0003)、Acetazolamide (HY-B0782) 或 MG132 (HY-13259) 联合处理时,会阻断 hCAII 的降解[1]

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

Western Blot Analysis[1]

Cell Line: HEK293 cells
Concentration: 0.005, 0.05, 0.5, 5, 50, 500, 5000, 10000, 15000 nM
Incubation Time: 0, 2, 6, 12, 24, 48 h
Result: Resulted in degradation of hCAII at concentrations as low as 50 pM, with near-complete degradation at 5 nM.
Showed no 'hook effect' at concentrations up to 15 μM.
Showed hCAII depletion beginning within 2 h, reaching maximal effect by 6 h, and sustaining degradation for 48 h.
分子量

639.76

Formula

C32H41N5O7S

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
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  • 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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PROTAC hCAII degrader-1
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HY-179467
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