化合物CC-885 T14893

Product Introduction
Bioactivity


英文名: CC-885

描述: CC-885 是一种 CRBN 蛋白调节剂，有抗肿瘤的潜能。

体外活性: The effect of CC-885 on cell proliferation in AML cell lines, THLE-2 and human PBMC is more powerful than Lenalidomide and Pomalidomide with IC50s>10 μM. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. Acute myeloblatlic leukemia (AML) cell lines, human liver epithelial cell line (THLE-2) and human peripheral blood mononuclear cells (PBMC) are treated with varying concentrations of CC-885, with IC50s of 10×-6-1 μM. To address whether the cereblon-dependent degradation of GSPT1 is responsible for the cytotoxic effects of CC-885, a GSPT1 mutant that retains its normal function, but loses CC-885-dependent cereblon binding, is used to distinguish the role of GSPT1 from that of other substrates. Overexpression of a resistant variant GSPT1Δ(1–138)/(G575N) completely abrogate the CC-885-induced anti-proliferation. Whereas overexpression of a CC-885-sensitive variant GSPT1Δ(1-138) only confer partial protection. Similar results are obtained in AML cell lines[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 67.5 mg/mL (153.10 mM)


关键字: Ligands for E3 Ligase | CC 885 | CC885 | E3 ligase-recruiting Moiety | Inhibitor | CC-885 | inhibit

相关产品: Thalidomide-O-amido-C3-NH2 TFA | SMER3 | (S,R,S)-AHPC-Me-C10-NH2 hydrochloride | CRBN modulator-1 | (S,R,S)-AHPC-PEG2-N3 | HaloPROTAC3 | Lenalidomide hemihydrate | (S,R,S)-AHPC-C10-NH2 | VH032 | Thalidomide-propargyl

相关库: ReFRAME Related Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Bioactive Compound Library

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