mcl

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

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 antagonist 1 is a Mcl-1 protein antagonist.

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

Mcl-1 Inhibitor 17 is a compound that functions as an inhibitor of the Mcl-1 protein, specifically designed for use in cancer and other disease research [1].

Bcl-2/Mcl-1-IN-3 is a Bcl-2/Mcl-1 inhibitor that acts on Mcl-1 (Ki: 0.14 μM) and Bcl-2 (Ki: 0.23 μM) and can be used in cancer research.

Bcl-2/Mcl-1-IN-2 is a Bcl-2 (Ki: 4.70 μM) and Mcl-1 (Ki: 0.88 μM) inhibitor.Bcl-2/Mcl-1-IN-2 can be used 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 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/BCL-2-IN-2 is a selective Mcl-1 and Bcl-2 inhibitor with potential antitumor activity for tumor research.

Mcl-1 inhibitor 6 is a potent, orally active chemical compound that selectively inhibits the myeloid cell leukemia 1 (Mcl-1) protein, with a high affinity (K d = 0.23 nM) and binding activity (K i = 0.02 μM). This compound exhibits exceptional selectivity over other members of the Bcl-2 family, including Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w (K d >10 μM). Notably, Mcl-1 inhibitor 6 demonstrates strong antitumor activity.

MCL-1/BCL-2-IN-3 is a selective and potent Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectiely.

MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective dual inhibitor of Mcl-1 and Bcl-2 with IC 50 s of 4.45 and 3.18 μM, respectively [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].

Bcl-2/Mcl-1-IN-1 is an inhibitor of Bcl-2 (Ki: 4.53 μM) and Mcl-1 (Ki: 1.19 μM).Bcl-2/Mcl-1-IN-1 can be used in cancer research.

MCL0129, a selective and non-peptidergic melanocortin 4 (MC4) receptor antagonist, is a potential treatment for cachexia.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115 and > 10 000 nM at MC4, MC3 and MC1 receptors respectively). Significantly reverses stress-induced anorexia but has no effect on food intake in free-feeding rats. Exhibits anxiolytic-like activity in vivo.

dMCL1-2 is a potent and selective myeloid leukemia 1 (MCL1) degrading agent based on PROTAC, which binds to MCL1 with a KD of 30 nM. dmcl-2 activates the apoptosis mechanism by degrading MCL1.This compound is unstable in powder form and other related salt forms are recommended.

SOMCL-863 is a selective and orally bioavailable c-Met inhibitor. It shows antitumor activity both in vitro and in vivo.

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

MDK-3345 is a reversible covalent inhibitor for Mcl-1.

MDK-3298 is a reversible covalent inhibitor of Mcl-1, a target of protein-protein interaction (PPI).

S63845 is a selective MCL-1 inhibitor(Kd: 0.19 nM)

UMI-77, a specific Mcl-1 inhibitor (Ki: 490 nM), has selectivity over other members of Bcl-2 family.

Triacetylresveratrol (Acetyl-trans-resveratrol) has anti-cancer activity,it inhibits the phosphorylation of STAT3 and NFκB, down-regulates Mcl-1, and up-regulates Bim and Puma in pancreatic cancer cells.

PROTAC Mcl1 degrader-1 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity. PROTAC Mcl1 degrader-1, a proteolysis targeting chimera (PROTAC), is a potently and selectively Mcl-1 inhibitor with an IC50 of 0.78 μM.

BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src.

Motixafortide TFA(664334-36-5,Free) (BKT140 TFA) is an antagonist of CXCR4 with IC50 of ～1 nM. It induces the apoptosis of AML blasts by down-regulating ERK, BCL-2, MCL-1 and cyclin-D1 via altered miR-15a 16-1 expression.

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

SD-36 is a selective and efficient STAT3 protein degrader (Kd=~50 nM) with antitumor activity that promotes growth inhibition and induces apoptosis by inhibiting Mcl-1 in gliomas.SD-36 inhibits the transcriptional activity of STAT3.

SC-2001 is a MCL-1 inhibitor. SC-2001 inhibits STAT3 phosphorylation through enhancing SHP-1 expression and induces apoptosis in human breast cancer cells. SC-2001 overcomes STAT3-mediated sorafenib resistance through RFX-1/SHP-1 activation in hepatocellu

Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with 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-26 is an effective and selective myeloid cell leukemia 1 inhibitor.

Mcl1-IN-4 is an inhibitor of Mcl1 ( IC50:0.2 μM).

Mcl1-IN-8 is an Mcl-1-PUMA interface inhibitor (Ki: 0.3 μM). In cancer cells, Mcl1-IN-8 shows dual activity on reducing PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis.

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

A-1210477 is an effective and specific MCL-1 and Bcl-2 inhibitor (Ki IC50: 0.454 26.2 nM).

A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).

Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.

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

Gossypol acetic acid (AT101), a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.

IMB-XH1 (Mcl1-IN-2) is a myeloid cell factor 1 (Mcl-1) inhibitor.

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.

ABBV-467, a selective MCL-1 inhibitor (K i : <0.01 nM), induces apoptosis and effectively promotes cancer cell death while inhibiting tumor growth in hematological malignancy models, including multiple myeloma [1].

NH2-C6-NH-Boc is a PROTAC linker. NH2-C6-NH-Boc can be used in the synthesis the Mcl-1 inhibitor based on PROTAC.