PROTAC EED degrader-1

CAS编号: 2639882-72-5
分子式: C₅₅H₆₀FN₁₁O₈S
分子量: 1054.20

有货

库存信息

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库存信息

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库存信息

关闭

货号 (SKU)	包装规格	是否现货
P647800-10mg	10mg	期货
P647800-25mg	25mg	期货
P647800-5mg	5mg	期货

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基本描述

规格或纯度	99%
英文名称	PROTAC EED degrader-1
生化机理	PROTAC EED degrader-1 is a von Hippel-Lindau -based PROTAC targeting EED with a pK D of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 ( PRC2 ) inhibitor ( pIC 50 =8.17) targeting the EED subunit.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	PROTAC EED degrader-1 is a von Hippel-Lindau -based PROTAC targeting EED with a pK D of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 ( PRC2 ) inhibitor ( pIC 50 =8.17) targeting the EED subunit In Vitro PROTAC EED degrader-1 (Compound PROTAC 2) binds to EED with a pK D of 9.02±0.09 and inhibits PRC2 function with a pIC 50 of 8.17±0.24. PROTAC EED degrader-1 (0.01-100 μM; 14 days) can potently inhibit proliferation of an EZH2 mutant DLBCL cell line Karpas422. PROTAC EED degrader-1 (0.1-3 μM; 48 hours) reduces the protein levels of EED, EZH2, H3K27me3 in Karpas422 cells. PROTAC EED degrader-1 (1 μM ; 1-24 h) promotes degradation of EED, EZH2, and SUZ12 in Karpas422 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: Karpas422 cells Concentration: 0.01, 0.1, 1, 10, 100μM Incubation Time: 4, 8, 12, 14 days Result: Reduced proliferation. GI 50 =0.045 uM (Day 14). Western Blot AnalysisCell Line: Karpas422 cells Concentration: 0.1, 1, and 3 μM Incubation Time: 48 hours Result: The protein levels of EED, EZH2, H3K27me3 was reduced. Western Blot AnalysisCell Line: Karpas422 cells Concentration: 1 μM Incubation Time: 1, 2, 4, 6, 8, 24 hours Result: EED protein levels decreased within 1-2 h of treatment. Form:Solid IC50& Target:VHL

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名称和识别符

Canonical SMILES	FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C4=C(C)N=C(CCC(NCCOC5=CC=C(OCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)C=C5)=O)C=C4)C9=NN=CN39
分子量	1054.20