inhibitor of mcl 1

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

BT2, a BCKDC kinase (BDK) inhibitor, exhibits an IC50 of 3.19 μM and functions as a potent, selective Mcl-1 inhibitor with a Ki value of 59 μM. Its interaction with BDK induces helix movements in the N-terminal domain, leading to BDK's dissociation from the branched-chain α-ketoacid dehydrogenase complex (BCKDC).

NH2-C6-NH-Boc is a PROTAC linker used in the synthesis of the Mcl-1 inhibitor [based on PROTAC].

API-1 (NSC-177223) is a potent inhibitor of Akt. It induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis .

Voruciclib is an orally active and selective CDK inhibitor (Ki: 0.626 nM-9.1 nM) that represses the expression of MCL-1 in multiple models of diffuse large B-cell lymphoma and effectively blocks CDK9, the transcriptional regulator of MCL-1.

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.

CMLD010509 (SDS-1-021) is a highly selective inhibitor of the oncogenic translation program that supports multiple myeloma (MM), targeting key oncoproteins such as MDM2, CCND1, MYC, MAF, and MCL-1.

Maritoclax (Marinopyrrole A) (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor, shows >8 fold selectivity than BCL-xl (IC50 > 80 μM),with an IC50 value of 10.1 μM.

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

MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 4.45 μM and 3.18 μM, respectively [1].

MCL-1/BCL-2-IN-2 is a potent and selective dual inhibitor of Bcl-2 and Mcl-1.

MCL-1/BCL-2-IN-3 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2, with IC50 values of 5.95 and 4.78 μM, respectively.

MCL-1/BCL-2-IN-4 is a selective and potent dual inhibitor of Mcl-1 and Bcl-2.

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-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.

Unesbulin (PTC596) is an orally active, selective inhibitor of B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1).

(R)-MIK665, the less active enantiomer of MIK665, is a specific inhibitor of Mcl-1 with an IC50 of 1.81 nM.

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.

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

Pyridoclax is an inhibitor of potential Mcl-1.

VU0661013 is an effective and selective inhibitor of MCL-1.

A-1155905 is an MCL-1 inhibitor with anticancer activity, demonstrating a half maximal inhibitory concentration (IC50) of 33.5 Nm and a dissociation constant (Ki) of 0.58 nM. This compound selectively binds to MCL-1 and possesses sufficient affinity to disrupt the MCL-1-Bim complex in live cells. The induction of death in MCL-1-dependent cell lines by A-1155905 is reliant on caspase proteins and occurs through apoptosis.

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.