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COA of KH-4-43

Description:

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.

Chemical Information

Catalog Novel inhibitors
Molecular Weight (MW) 422.744
Molecular Formula C19H10ClF3N2O4
Storage 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Handling:

Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.