KH-4-43 | E3 CRL4 inhibitor | Probechem Biochemicals

Chemical Structure : KH-4-43

加入收藏

KH-4-43 (E3 CRL4 inhibitor)

货号: PC-72548Not For Human Use, Lab Use Only.

KH-4-43 is a small moelcule E3 CRL4 inhibitor and exhibits antitumor potential, directly and selectively binds to the purified E3 ROC1-CUL4A CTD complex with Kd of 83 nM.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

KH-4-43 is a small moelcule E3 CRL4 inhibitor and exhibits antitumor potential, directly and selectively binds to the purified E3 ROC1-CUL4A CTD complex with Kd of 83 nM.
KH-4-43 weakly binds to the purified, highly related E3 ROC1-CUL1 CTD complex with Kd of 9.4 uM, >100-fold less potent than ROC1-CUL4A CTD, showed little effect on Ub thiol ester formation with E1/E2 Cdc34.
KH-4-43 inhibited the ubiquitination of CK1α by CRL4CRBN in vitro. Treatment of cells with KH-4-43 caused accumulation of the E3 CRL4 substrate CDT1.
KH-4-43 inhibited cell viability against a panel of tumor lines, NB-4, MV4-11, OVCAR-3, and CAPAN-2 cell with IC50 of 1.8, 3.0, 3.9, and 4.8 uM, respectively.
KH-4-43 suppress the growth of human tumor xenografts in mice.

物理化学性质&存储条件

分子量	422.744
分子式	C19H10ClF3N2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-[1-(4-Chlorophenyl)-1H-pyrazol-4-yl]-7,8-dihydroxy-2-(trifluoromethyl)-4H-1-benzopyran-4-one

参考文献

1. Kenneth Wu, et al. Proc Natl Acad Sci U S A. 2021 Feb 23;118(8):e2007328118.