mcl 1 antagonist 1

Mcl-1 antagonist 1 is an inhibitor of the Mcl-1 protein.

(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively).

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a/16-1 expression.

Mcl-1 inhibitor20 (compound 47) is an Mcl-1 antagonist with anti-leukemia properties. It binds to the BH3 docking groove of Mcl-1 (Ki=24 nM), occupies the P1 pocket, and interacts with Lys234 and Val249. Mcl-1 inhibitor20 also exhibits good microsomal stability, favorable pharmacokinetic properties, and low cardiotoxicity.

ASTX295 is a selective mouse double minute 2 (MDM2) antagonist with an IC50 value of less than 1 nM. It specifically inhibits the interaction between MDM2 and p53, reactivating wild-type (WT) TP53, which subsequently induces the expression of related transcriptional targets, leading to cell death and cell cycle arrest. ASTX295 holds potential for research in lymphoid malignancies such as diffuse large B-cell lymphoma (DLBCL), mantle cell lymphoma (MCL), and T-cell lymphoma.

UNBS-1450 is a sodium channel antagonist. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin, it is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induce