mcl-1-in-3

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

Bcl-2/Mcl-1-IN-3 is a Bcl-2/Mcl-1 inhibitor, targeting Mcl-1 (Ki: 0.14 μM) and Bcl-2 (Ki: 0.23 μM), suitable for cancer research.

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.

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 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).

AZD5991 is a potent and selective Mcl-1 inhibitor aimed at treating hematological cancers. As a well-designed macrocyclic compound, AZD5991 exhibits sub-nanomolar affinity for Mcl-1. It primarily inhibits the myeloid cell leukemia-1 protein (Mcl-1; Bcl2-L-3), showing potential pro-apoptotic and anti-tumor activity. AZD5991 binds to Mcl-1, preventing its interaction with certain pro-apoptotic proteins, leading to apoptosis in cells overexpressing Mcl-1.

3’-Me Meayamycin D is a splice modulator that targets SF3B1 and PHF5A, affecting the pre-mRNA splicing process and downregulating MCL-1 expression. It inhibits the proliferation of cancer cell lines HCT116, SW48, A549, DMS53, and DMS114, with a GI50 range of 4.6-7.2 nM. In mice, it demonstrates good plasma stability with a half-life of 16 hours.

PDGFRA/CAIX/XII-IN-1 is a multi-target inhibitor targeting PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA and Ki values of 93.3 nM and 80.0 nM against CA IX and CA XII respectively. It targets and binds to the ATP-binding pocket of PDGFRA, thereby blocking the activation of downstream signaling pathways such as STAT3, AKT and ERK1/2. It induces G0/G1 phase cell cycle arrest and initiates endogenous apoptotic procedures, manifested as cleavage and activation of PARP-1, caspase-9 and caspase-3, upregulation of caspase 3/7 activity and inhibition of Mcl-1 protein expression. It exerts significant anti-proliferative effects in eosinophilic leukemia cells and can serve as a candidate tool compound for mechanism and efficacy research of leukemia.

Mcl-1-IN-20 (Compound 26d) is an Mcl-1 inhibitor displaying Ki values of 0.59 μM for Mcl-1, 6.6 μM for Bcl-xL, and 3.6 μM for Bcl-2. It exhibits significant antiproliferative activity against pancreatic cancer cells and induces apoptosis in BxPC-3 cells. Mcl-1-IN-20 is applicable in pancreatic cancer research.

Mcl-1-IN-16 is an effective macrolide inhibitor of myeloid cell leukemia 1 (Mcl-1) with a Ki of less than 0.08 nM. It demonstrates over 50,000-fold selectivity for Mcl-1 compared to other anti-apoptotic Bcl-2 family members, Bcl-2 and Bcl-xL. Mcl-1-IN-16 activates caspase-3/7, thereby inducing apoptosis. In tumor xenograft mouse models derived from lung cancer, it achieves tumor regression. Mcl-1-IN-16 is useful for research on solid tumors, including non-small cell lung cancer (NSCLC).

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

Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.

3-Tridecylphenol is a type of cardanol. It can be isolated from K. hookeriana and demonstrates Ki values of >23 μM in BclxL/Bak displacement assays and >33 μM in Mcl-1/Bid assays. This compound is applicable in cancer research.