Mcl-1 Inhibitor

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a K_d of 0.19 nM for human MCL1.

ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

A-1331852 is an orally available BCL-XL selective inhibitor with a K_i of less than 10 pM.

BT2 is a BCKDC kinase (BDK) inhibitor with an IC₅₀ of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a K_i value of 59 μM.

AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC₅₀ of 0.7 nM in FRET assay and a K_d of 0.17 nM in surface plasmon resonance (SPR) assay.

PROTAC B-Raf degrader 1 is a PROTAC degrader targeting B-Raf, which recruits the ubiquitin-proteasome system to accelerate B-Raf degradation and reduce the expression of downstream Mcl-1. PROTAC B-Raf degrader 1 inhibits cancer cell proliferation, arrests cell cycle and induces apoptosis. PROTAC B-Raf degrader 1 can be used in breast cancer-related research.

TC11 is a MCL1 degrader and apoptosis inducer. TC11 induces sustained CDK1 activation to phosphorylate and degrade MCL1, activates caspase-3, -8, and -9, inhibits centrosomal-regulatory NPM function to block centrosomal clustering, and triggers apoptosis independent of the cereblon pathway. TC11 blocks tumor cell proliferation in vitro and acts against tumor xenografts in vivo. TC11 can be used for the research of multiple myeloma.

MIK665 (S-64315), derived from S63845, is a myeloid cell leukemia sequence 1 (MCL1) inhibitor. MIK665 has an IC₅₀ of 1.81 nM for MCL1.

Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-X_L, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC₅₀s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.

Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a K_i of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.

UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC₅₀=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with K_i of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.

A-1210477 is a potent and selective inhibitor of MCL-1 with a K_i of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.

PROTAC Bcl2 degrader-1 (Compound C5) is a PROTAC based on Cereblon ligand, which potently and selectively induces the degradation of Bcl-2 (IC₅₀, 4.94 μM; DC₅₀, 3.0 μM) and Mcl-1 (IC₅₀, 11.81 μM) by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1/Bcl-2 dual inhibitor Nap-1.

PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM.

TW-37 is a potent Bcl-2 inhibitor with K_i values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.

(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with K_is of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a K_i of 0.13 nM.

SHP2-D26 is a SHP2 PROTAC degrader with DC₅₀ values of 6.0 nM (KYSE520 cells) and 2.6 nM (MV4;11 cells), respectively. SHP2-D26 inhibits ERK phosphorylation, upregulates Bim levels, downregulates Mcl-1 levels, and induces cell cycle arrest and apoptosis. SHP2-D26 can be used in studies related to esophageal cancer, acute myeloid leukemia and non-small cell lung cancer.

Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC₅₀s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression.

VU661013 is a potent and selective MCL-1 inhibitor.