inhibitor of mcl1

MIM1 (Inhibitor of Mcl-1) is an myeloid cell factor 1 (Mcl-1) inhibitor.

S63845 is a selective myeloid leukemia 1(MCL1) inhibitor that binds to human MCL1 with a Kd of 0.19 nM.

AZD-5991 Racemate is the racemate of AZD-5991. (Rac)-AZD-5991 is a novel Mcl-1 inhibitor with IC50 <3 nM in FRET assay and induces upregulation of BCL2,BCL-XL, CMYC and MCL1 in AML cell lines.

Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor with Kis of 0.06 μM and 4.2 μM for Mcl-1 and Bcl-2, respectively.

Mcl1-IN-12 has anti-tumor activity.It is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively.

Mcl1-IN-4 is an Mcl1 inhibitor with an IC50 of 0.2 μM.

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) inhibitor, exhibiting an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.

Tapotoclax (AMG-176) is an orally active MCL1 inhibitor for the study of myeloid leukemia.

Mcl1-IN-3 is an Mcl1 inhibitor. It has an IC50 and Ki of 0.67 and 0.13 μM, respectively.

CLZ-8 (Mcl1-IN-8) is an orally active inhibitor of Mcl-1-PUMA (p53 up-regulated mediator of apoptosis) with radioprotective properties.CLZ-8 ameliorates radiation-induced HUVEC cell damage and reduces apoptosis counts, and inhibits radiation-induced overexpression of PUMA.

CDK9-IN-33 (compound C35) is a potent, selective, and orally bioavailable CDK9 inhibitor with IC50 values of 17.44 nM for CDK9, 160 nM for CDK7, 316.30 nM for CDK2, 1771.00 nM for CDK4, and >10000 nM for CDK6. This compound induces apoptosis (cell apoptosis) and reduces the protein expression of RPB1 CTD Ser2, RPB1, and MCL1, exhibiting antitumor activity.

AZ5576 racemate is a racemic mixture of AZ5576 isomers. AZ5576 is a potent, highly selective, and orally bioavailable inhibitor of Cdk9 that inhibits Cdk9 enzyme activity with an IC50 <5nM and decreases phosphorlyation of Ser2-RNAPII in cells with an IC50 of 96nM. In the MLL-fusion containing acute myeloid leukemia (AML) line, MV411, short-term treatment with AZ5576 led to a rapid dose-dependent decrease in pSer2-RNAPII with concomitant loss of Mcl1 mRNA and protein, resulting in the cleavage and activation of caspase 3 and loss of cell viability.

BRD-810 is a highly selective MCL1 inhibitor (Kd=0.3 nM) capable of inducing tumour cell apoptosis, suitable for studying haematological malignancies and solid tumours. BRD-810 binds the BH3 groove of MCL1, activates Caspase, and disrupts the MCL1-BAK complex in cancer cells (IC50=1.2 nM).

TC11 (1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11) is a potent inhibitor of tumor cell proliferation and an inducer of apoptosis via activation of caspase-3, 8 and 9.