mcl

Cladribine (2CdA), an adenosine deaminase inhibitor, is utilized in the treatment of lymphoproliferative diseases.

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.

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).

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.

PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC), a selective Mcl-1 inhibitor. By hijacking the CRBN ubiquitin ligase to form a ternary complex with the target protein, it induces Mcl-1 ubiquitination. It can be used for cancer research.

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.

Mcl1-IN-1 is a myeloid cell factor 1 inhibitor (IC50=2.4 µM).

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

Mcl-1 inhibitor22 (Example 36) is an MCL-1 inhibitor that suppresses its anti-apoptotic function by blocking the interaction between MCL-1 and pro-apoptotic proteins. It exhibits antiproliferative activity against various cancer cell lines and can be utilized for cancer research.

(-)-Mcl-1 inhibitor 22 (compound 38) is an agent that targets Mcl-1 and functions by blocking the interaction between Mcl-1 and pro-apoptotic proteins, thereby hindering Mcl-1's anti-apoptotic activity. It is applicable in cancer research.

(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.

(-)-Mcl-1 inhibitor 21 (Example 1-38) is an Mcl-1 inhibitor with an IC50 of 7.51 μM. It exhibits pro-apoptotic and anti-proliferative activity against SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.

Mcl-1 inhibitor21 (Example 1-36) is an Mcl-1 inhibitor with an IC50 of 328 nM. It exhibits pro-apoptotic and anti-proliferative activity against SUDHL5 and SUDHL10 cell lines, making it applicable for cancer research.

(+)-Mcl-1 inhibitor 21 (Example 1-37) is a chemical compound that acts as an Mcl-1 inhibitor with an IC50 value of 172 nM. It demonstrates pro-apoptotic and antiproliferative activities in SUDHL5 and SUDHL10 cell lines, making it useful for cancer research.

Mcl-1 inhibitor18 (compound 57) is an inhibitor of myeloid cell leukemia 1 (Mcl-1) and is utilized in cancer research.

Mcl-1-IN-17 (Compound 25) is an orally active inhibitor of myeloid cell leukemia 1 protein (Mcl-1), with a Ki of less than 0.08 nM. It exhibits significant antiproliferative activity with GI50 values of 39 nM in H929 cells and 105 nM in A427 cells, and it inhibits apoptosis. This compound is suitable for research in hematological and solid tumors.

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).