mcl-1

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 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).

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

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 6 is a potent, orally active small molecule that selectively targets the anti-apoptotic protein myeloid cell leukemia 1 (Mcl-1). Mcl-1 inhibitor 6 binds with high affinity, with a dissociation constant (K d) of 0.23 nM, and exhibits binding activity with a K i of 0.02 μM. Mcl-1 inhibitor 6 displays exceptional selectivity over other anti-apoptotic Bcl-2 family proteins, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, all of which display binding constants greater than 10 μM. Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity in preclinical models, highlighting its potential as a therapeutic candidate in oncology.

Mcl-1 inhibitor20 (compound 47) is an Mcl-1 antagonist with anti-leukemia properties. It binds to the BH3 docking groove of Mcl-1 (Ki=24 nM), occupies the P1 pocket, and interacts with Lys234 and Val249. Mcl-1 inhibitor20 also exhibits good microsomal stability, favorable pharmacokinetic properties, and low cardiotoxicity.

Mcl-1 inhibitor19 (compound 26) binds to Mcl-1 with a Ki of 86 pM and inhibits the growth of H929 cells with a GI50 of 43 nM.

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 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.

Mcl-1 Inhibitor 12 (Example 10), with a K i of 0.22 nM, functions as an MCL-1 inhibitor. It is utilized in cancer research [1].

Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].

Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential for use in anticancer research [1].

Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].

Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells. This compound exhibits antitumor activity and may be utilized as a monotherapy or in combination with ABT-199 [1].

Mcl-1 inhibitor 17 is an effective inhibitor of the Mcl-1 protein. Mcl-1 is a critical anti-apoptotic member of the Bcl-2 family, frequently overexpressed in various malignancies, where it suppresses apoptosis by sequestering pro-apoptotic proteins such as Bak and Bax. Mcl-1 inhibitor 17 functions by competitively binding to the BH3-binding groove of Mcl-1, thereby releasing pro-apoptotic factors and restoring apoptotic sensitivity in cancer cells. This compound is utilized for research into cancer and other diseases associated with Mcl-1 dysregulation.

Mcl-1 inhibitor10 (compound 43) is a relatively potent MCL-1 inhibitor with an IC50 of 0.67 μM. It interacts with a specific binding site on the MCL-1 protein, disrupting its pro-survival signals and inducing apoptosis in cancer cells. This compound is useful for research on MCL-1-dependent cancers.