Search Result
Results for "
MCL-1 inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-155472
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 17 is a Mcl-1 protein inhibitor. Mcl-1 inhibitor 17 can be used for the research of cancer and other diseases .
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- HY-145826
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112 .
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- HY-148899
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 10 (compound 43) is a relatively strong MCL-1 inhibitor (IC50=0.67 μM). Mcl-1 inhibitor 10 interacts with specific binding sites of MCL-1 protein to block the pro-survival signal of MCL-1 and push cancer cells into apoptosis. Mcl-1 inhibitor 10 can be used in the study of MCL-1 dependent cancers .
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- HY-153423
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 12 (Example 10) is a MCL-1 inhibitor (Ki: 0.22 nM). Mcl-1 inhibitor 12 can be used for the research of cancers .
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- HY-153423A
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 13 (Example 9) is a MCL-1 inhibitor (Ki: 8.2 nM). Mcl-1 inhibitor 13 can be used for the research of cancers .
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- HY-159588
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 20 (compound 47) is a Mcl-1 inhibitor with anti-leukemic effects. Mcl-1 inhibitor 20 can bind to the BH3 binding groove of Mcl-1 (Ki=24 nM), occupy the P1 pocket in Mcl-1, and form interactions with Lys234 and Val249. Mcl-1 inhibitor 20 has good microsomal stability, pharmacokinetic characteristics and low cardiotoxicity .
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- HY-154962
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 15 (Compound (Ra)-15) is a Mcl-1 inhibitor (Ki: 0.02 nM). Mcl-1 inhibitor 15 can be used for research of cancer .
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- HY-162780
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 19 (compound 26) binds to Mcl-1, with the Ki of 86 pM. Mcl-1 inhibitor 19 inhibits growth in H929 cells with the GI of 43 nM .
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- HY-148203
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity .
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- HY-155012
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 16 (Compound 9) is a mitochondrial targeting Platinum-based inhibitor of Mcl-1. Mcl-1 inhibitor 1 induces Bax/Bak-dependent apoptosis in cancer cells. Mcl-1 inhibitor 16 can be used alone or together with ABT-199 (HY-15531) and shows anti-tumor activity .
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- HY-145825
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 7 is a potent Mcl-1 inhibitor, example 35, extracted from patent WO2020097577A .
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- HY-163293
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 18 (compound 57) is a myeloid cell leukemia 1 (Mcl-1) inhibitor, and can be used for study of cancer .
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- HY-132307
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Bcl-2 Family
Apoptosis
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Cancer
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Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent .
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- HY-133015
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 3 (compound 1) 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 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity ..
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- HY-154961
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 14 (Compound (Ra)-10) is an inhibitor of myeloid cell leukemia-1 (MCL-1) with an Ki of 0.018 nM and can be used for anticancer research .
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- HY-16695
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inhibitor of MCL-1
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Bcl-2 Family
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Cancer
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MIM-1 is an inhibitor of myeloid cell factor 1 (Mcl-1).
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- HY-145825A
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Bcl-2 Family
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Cancer
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(E)-Mcl-1 inhibitor 7 (Example 34) is a Mcl-1 inhibitor (Ki: <1 nM, IC50: <500 nM). (E)-Mcl-1 inhibitor 7 can be used for research of cancers .
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- HY-164453
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Bcl-2 Family
Apoptosis
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Cancer
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A-1248767 is a MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) with anticancer activity. A-1248767, a derivative of A-1210477 (HY-12468), binds to MCL-1 with high affinity, induces the increase of intracellular MCL-1 protein, and promotes tumor cell apoptosis .
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- HY-164452
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Bcl-2 Family
Apoptosis
Caspase
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Cancer
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A-1155905 is a MCL-1 inhibitor (IC50=33.5 nM; Ki=0.58 nM) with anticancer activity. A-1155905 selectively binds to MCL-1 with sufficient affinity to disrupt the MCL-1-bim complex in living cells. A-1155905-induced death of MCL-1-dependent cell lines is caspase-dependent and occurs via apoptosis .
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- HY-115928
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Bcl-2 Family
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Cancer
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M24 is a Mcl-1 selective inhibitor. M24 exhibits good binding affinity against Mcl-1 with Ki value of 0.33 μM. M24 exhibits good anti-proliferative activity and induce apoptosis in HepG2 cells .
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- HY-159513
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2/Mcl-1-IN-4 (compound 20) is a dual inhibitor targeting Bcl-2 (Ki=0.49 μM) and Mcl-1 (Ki=0.51 μM). Bcl-2/Mcl-1-IN-4 significantly inhibits cancer cell proliferation and effectively induces apoptosis in U937 cells. Bcl-2/Mcl-1-IN-4 can be used in cancer research .
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- HY-122721
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Bcl-2 Family
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Cancer
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Mcl1-IN-5 (compound 21) is a MCL-1 inhibitor. Mcl1-IN-5 can be used for the research of cancers .
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- HY-123564
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Others
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Others
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Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.
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- HY-111467
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- HY-16669
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Bcl-2 Family
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Cancer
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Mcl1-IN-1 is an inhibitor of myeloid cell factor 1 (Mcl-1) (IC50=2.4 µM).
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- HY-12527
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- HY-12468
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Bcl-2 Family
Apoptosis
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Cancer
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A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM . A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner .
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- HY-100762
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Bcl-2 Family
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Cancer
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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 .
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- HY-128607
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Bcl-2 Family
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Cancer
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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 .
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- HY-112859
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- HY-18628
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UMI-77
2 Publications Verification
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Bcl-2 Family
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Cancer
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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 Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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- HY-100763
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Bcl-2 Family
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Cancer
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Mcl1-IN-12 (Compound F) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively. Anti-tumor activity .
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- HY-163681
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- HY-100741
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S63845
Maximum Cited Publications
78 Publications Verification
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Bcl-2 Family
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Cancer
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S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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- HY-111468
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Bcl-2 Family
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Cancer
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Mcl1-IN-3 is an inhibitor of Mcl1 extracted from patent WO2015153959A2, compound example 57; has an IC50 and Ki of 0.67 and 0.13 μM, respectively.
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- HY-125877
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PROTACs
Bcl-2 Family
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Cancer
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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 .
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- HY-18628S
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Isotope-Labeled Compounds
Bcl-2 Family
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Cancer
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UMI-77-d4 is the deuterium labeled UMI-77. 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 Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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- HY-161732
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Bcl-2 Family
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Cancer
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GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL .
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- HY-129700
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Bcl-2 Family
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Cancer
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MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor .
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- HY-129702
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Bcl-2 Family
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Cancer
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MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor .
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- HY-162858
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Caspase
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Cancer
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BRD-810 is a highly selective MCL1 inhibitor. BRD-810 can bind to the BH3 groove of MCL1 and block the sequestration of pro-apoptotic proteins, quickly inducing caspase activation in MCL1-dependent cell lines. BRD-810 shows anti-tumor activity in models of blood cancers and solid tumors .
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- HY-12422A
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CDK
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Cancer
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Voruciclib hydrochloride is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib hydrochloride potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib hydrochloride represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
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- HY-12422
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CDK
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Cancer
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Voruciclib is an orally active and selective CDK inhibitor with Ki values of 0.626 nM-9.1 nM. Voruciclib potently blocks CDK9, the transcriptional regulator of MCL-1. Voruciclib represses expression of MCL-1 in multiple models of diffuse large B-cell lymphoma (DLBCL) .
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- HY-101565
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AMG-176
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Bcl-2 Family
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Cancer
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Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM .
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- HY-101533A
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Bcl-2 Family
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Cancer
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AZD-5991 Racemate is the racemate of AZD-5991. AZD-5991 Racemate is a Mcl-1 inhibitor with an IC50 of <3 nM in FRET assay.
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- HY-112218
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S-64315
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Bcl-2 Family
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Cancer
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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 .
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- HY-112218A
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Bcl-2 Family
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Cancer
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(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special Mcl-1 inhibitor with an IC50 of 1.81 nM.
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- HY-109184
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AMG 397
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Bcl-2 Family
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Cancer
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Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer .
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- HY-129701
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Bcl-2 Family
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Cancer
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MCL-1/BCL-2-IN-3 (Compound 2) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectively .
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- HY-100741A
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Others
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Cancer
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(S,R)-S63845 is the isomer of S63845 (HY-100741), and can be used as an experimental control. S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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- HY-100741C
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Others
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Cancer
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(R,R)-S63845 is the isomer of S63845 (HY-100741), and can be used as an experimental control. S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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- HY-12020
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TW-37
2 Publications Verification
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Bcl-2 Family
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Cancer
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TW-37 is a potent Bcl-2 inhibitor with Ki values of 260, 290 and 1110 nM for Mcl-1, Bcl-2 and Bcl-xL, respectively.
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- HY-129681
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Bcl-2 Family
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Cancer
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MCL-1/BCL-2-IN-2 (Compound Nap-1) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor with IC50s of 4.45 and 3.18 μM, respectively .
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- HY-144430
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Bcl-2 Family
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Cancer
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Bcl-2/Mcl-1-IN-1 (compound 3) is a Bcl-2/Mcl-1 inhibitor, with Kis of 1.19 μM and 4.53 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-1 can be used for the research of cancer .
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- HY-144431
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Bcl-2 Family
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Cancer
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Bcl-2/Mcl-1-IN-3 (compound 1) is a Bcl-2/Mcl-1 inhibitor, with Kis of 0.14 μM and 0.23 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-3 can be used for the research of cancer .
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- HY-144428
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Bcl-2 Family
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Cancer
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Bcl-2/Mcl-1-IN-2 (compound 2) is a Bcl-2/Mcl-1 inhibitor, with Kis of 0.88 μM and 4.70 μM for Mcl-1 and Bcl-2, respectively. Bcl-2/Mcl-1-IN-2 can be used for the research of cancer .
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- HY-101533
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Bcl-2 Family
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Cancer
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AZD-5991 is a potent and selective Mcl-1 inhibitor with an IC50 of 0.7 nM in FRET assay and a Kd of 0.17 nM in surface plasmon resonance (SPR) assay .
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- HY-15613
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Marinopyrrole A
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Bcl-2 Family
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Cancer
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Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
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- HY-150507
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Bcl-2 Family
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Cancer
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JNJ-4355 is a highly potent MCL-1 (myeloid cell leukemia-1) inhibitor, with KI of 18 pM. JNJ-4355 shows antitumor activity .
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- HY-115529
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Bcl-2 Family
Apoptosis
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Cancer
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(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells .
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- HY-112591
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Apoptosis
HIV
Wnt
Bcl-2 Family
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Cancer
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NSC260594 induces Apoptosis. NSC260594 binds the shallow groove of the Mcl-1 protein, and inhibits Mcl-1 expression through down-regulation of Wnt signaling proteins. NSC260594 can also recognize G9-G10-A11-G12 RNA tetraloop of HIV and prevent the binding of the Gag protein within the 5’-UTR. NSC260594 inhibits tumor growth, and can be used for research of Triple-negative breast cancers (TNBCs) .
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- HY-149672
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Bcl-2 Family
Apoptosis
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Cancer
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ABBV-467 is a selective MCL-1 inhibitor (Ki: <0.01 nM). ABBV-467 induces apoptosis. ABBV-467 induces cancer cell death and inhibits tumor growth in models of hematological malignancies, such as multiple myeloma .
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- HY-161274
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Bcl-2 Family
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Cancer
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Bfl-1-IN-1 (Compound 15) is a potent and selective Bfl-1 inhibitor. Bfl-1-IN-1 inhibits Bfl-1 and Mcl-1 with Kis of 0.63 and 6.77 μM, respectively .
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- HY-101533B
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Bcl-2 Family
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Cancer
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AZD-5991 S-enantiomer is the less active enantiomer of AZD-5991. AZD-5991 S-enantiomer is a Mcl-1 inhibitor with an IC50 of 6.3 μM in FRET assay and a Kd of 0.98 μM in surface plasmon resonance (SPR) assay.
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- HY-119009
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JAK
STAT
NF-κB
Bcl-2 Family
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Cancer
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TM-233 is an inhibitor of the JAK/STAT and NF-κB signaling pathways, exhibiting significant antitumor activity. TM-233 reduces the expression of the anti-apoptotic protein Mcl-1 by inhibiting the phosphorylation of JAK2 and STAT3, and regulates its transcription by directly binding to the Mcl-1 gene promoter. Additionally, TM-233 prevents the translocation of NF-κB from the cytoplasm to the nucleus by inhibiting its DNA-binding activity, thereby reducing nuclear NF-κB expression. TM-233 shows potential in overcoming Bortezomib (HY-10227) resistance and can be applied in research related to multiple myeloma .
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- HY-160438B
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Others
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Cancer
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PBX-7011 TFA is a derivative of camptothecin (HY-16560), which inhibits expressions of the cancer related survival genes DDX5, Survivin, Mcl-1 and XIAP in cells FaDu, degrades DDX5 proteins and exhibits anticancer activity .
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- HY-120113
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Others
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Others
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SC-2001 is a compound structurally related to obatoclax that has better antitumor effects than obatoclax in liver cancer cell lines, downregulating Mcl-1 protein levels, inhibiting STAT3 phosphorylation, inducing apoptosis, and enhancing SHP1 expression and activity.
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- HY-W008296
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PROTAC Linkers
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Cancer
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NH2-C6-NH-Boc is a PROTAC linker which refers to the alkyl/ether composition. NH2-C6-NH-Boc can be used in the synthesis the Mcl-1 inhibitor based on PROTAC .
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- HY-125876
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PROTACs
Bcl-2 Family
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Cancer
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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 (Blue: CRBN ligand, Black: linker；Pink: Mcl-1/Bcl-2 inhibitor, Nap-1).
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- HY-W689801
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Bcl-2 Family
Apoptosis
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Cancer
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A-1208746 is an inhibitor for MCL-1, with a Ki of 0.454 nM. A-1208746 activates caspase-3/-7, induces apoptosis in cell H929, and decreases mitochondrial membrane potential. A-1208746 synergies with Navitoclax (HY-10087), and can be used in cancer research .
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- HY-19551
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ApoG2
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Bcl-2 Family
Apoptosis
Autophagy
Fungal
ROS Kinase
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Infection
Cancer
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Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with Ki values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-XL, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy . Apogossypolone also has antifungal activity .
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- HY-155153
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Apoptosis
CDK
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Others
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CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research .
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- HY-116532
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Bcl-2 Family
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Cancer
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YCW-E11 is a Bcl-2, and Mcl-1 inhibitor with Ki values of 0.83 and 0.33 μM, respectively. YCW-E11 induces cell apoptosis through the mitochondrial pathway and exhibits antitumor activity. YCW-E11 can be utilized in cancer research .
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- HY-15191
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BI-97C1
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Bcl-2 Family
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Cancer
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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 .
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- HY-112041
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PTC596
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BMI1
Apoptosis
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Cancer
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Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity .
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- HY-167881
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Bcl-2 Family
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Cancer
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MLS-0053105, a chloromaleimide, is a selective BFL-1 inhibitor with an IC50 of 0.4 µM for Bfl-1/F-Bid. MLS-0053105 shows over 10 times less potent inhibition of Bcl-W, Bcl-2, and Bcl-XL and no activity against Bcl-B and Mcl-1 .
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- HY-114855
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BT2
4 Publications Verification
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Bcl-2 Family
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Metabolic Disease
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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 Ki value of 59 μM .
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- HY-158783
-
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Ceramidase
Bcl-2 Family
LPL Receptor
Apoptosis
|
Neurological Disease
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SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
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-
- HY-149495
-
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PROTACs
CDK
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Cancer
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CP-07 is a potent and selective PROTACCDK9 degrader (DC50: 43 nM). CP-07 inhibits 22RV1 cell proliferation (IC50: 62 nM) and colony formation by down-regulating Mcl-1 and c-Myc. CP-07 inhibits 22RV1 xenograft tumor growth. CP-07 can be used for research of prostate cancer .
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- HY-138697
-
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VOB560
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Bcl-2 Family
Apoptosis
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Cancer
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S65487 (VOB560), a potent and selective BCL-2 inhibitor, is a proagent of S55746. S65487 is also active on BCL-2 mutations, such as G101V and D103Y. S65487 has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 induces apoptosis and has anticaner activities .
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- HY-138697B
-
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VOB560 hydrochloride
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Bcl-2 Family
Apoptosis
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Cancer
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|
S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 hydrochloride is also active on BCL-2 mutations, such as G101V and D103Y. S65487 hydrochloride has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 hydrochloride induces apoptosis and has anticaner activities .
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- HY-111537
-
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Others
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Others
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rel-AZ5576 is a selective CDK9 inhibitor with the activity of downregulating Mcl-1 and MYC mRNA transcription and protein expression in diffuse large B-cell lymphoma by inhibiting CDK9, promoting MYC protein turnover, reducing MYC phosphorylation on the stable Ser62 residue and downregulating MYC transcriptional targets, inhibiting the growth of diffuse large B-cell lymphoma cell lines in vitro and in vivo and independent of the cell origin.
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-
- HY-15163A
-
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FLT3
JAK
CDK
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Cancer
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Zotiraciclib hydrochloride is a novel small molecule multi-target enzyme inhibitor with activity in inhibiting tumor growth. Zotiraciclib hydrochloride exerts its anti-tumor effect by reducing the level of Myc through inhibiting cyclin-dependent kinase 9 (CDK9). Zotiraciclib hydrochloride may be useful for inhibiting cancers that cross the blood-brain barrier. The high protein level of MCL-1 of Zotiraciclib hydrochloride is associated with survival, suggesting that it may serve as a prognostic factor and inhibitory target in further studies .
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- HY-146097
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P-glycoprotein
Apoptosis
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Cancer
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RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property .
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- HY-N0087
-
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Beta-Guttiferrin
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Bcl-2 Family
Autophagy
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Cancer
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Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, 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.
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- HY-138697A
-
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VOB560 sulfate
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Bcl-2 Family
Apoptosis
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Cancer
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|
S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a proagent of S55746. S65487 sulfate is also active on BCL-2 mutations, such as G101V and D103Y. S65487 sulfate has poor affinity with MCL-1, BFL-1 and BCL-XL. S65487 sulfate induces apoptosis and has anticaner activities .
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- HY-161733
-
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|
Bcl-2 Family
|
Cancer
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GQN-B37-Me is a MCL-1 inhibitor. GQN-B37-Me induces caspase-dependent apoptosis. GQN-B37-Me exhibits noteworthy cytotoxicity in H929 (IC50 = 3.71 μM) and MV-4-11 (IC50 = 5.57 μM) cells. GQN-B37-Me can be used for the research of leukemia .
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- HY-76474A
-
|
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Apoptosis
Syk
|
Inflammation/Immunology
Cancer
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BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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-
- HY-N8146
-
|
|
STAT
|
Infection
Cancer
|
|
Bruceantinol, a quassinoid isolated from Brucea javanica, inhibits pepper mottle virus in pepper . Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50=2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc .
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-
- HY-76474
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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-
- HY-12826
-
|
|
Beta-lactamase
Bcl-2 Family
Bacterial
|
Cancer
|
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1) . IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively .
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-
- HY-119271
-
|
SDS-1-021
|
c-Myc
Apoptosis
|
Cancer
|
|
CMLD010509 (SDS-1-021) is a highly specific inhibitor of the oncogenic translation program supporting multiple myeloma (MM)-including key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. CMLD010509 (SDS-1-021) shows an IC50 below 10 nM for most MM cell lines and induces apoptosis. CMLD010509 (SDS-1-021) is a potent and selective translation inhibitor through an eIF4E phosphorylation-independent mechanism .
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- HY-155245
-
|
|
CDK
Bcl-2 Family
|
Cancer
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A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation .
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- HY-149007
-
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|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-11 (7a) is a selective STAT3 inhibitor that inhibits the phosphorylation of STAT3 at site pTyr705. STAT3-IN-11 inhibits the phosphorylation of downstream genes (Survivin and Mcl-1) without affecting its upstream tyrosine kinases (Src and JAK2) levels and p-STAT1 expression. STAT3-IN-11 can induce cancer cell apoptosis, which is potential for the discovery of effective STAT3 inhibitors and antitumor agents against cancers .
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- HY-N0087R
-
|
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
Gambogic Acid (Standard) is the analytical standard of Gambogic Acid. This product is intended for research and analytical applications. Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, 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.
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-
- HY-164468
-
|
|
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
|
|
Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087) .
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-
- HY-164460
-
|
|
Pim
|
Cancer
|
|
AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
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-
- HY-13559
-
|
Azaspirane
|
Apoptosis
|
Cancer
|
|
Atiprimod (Azaspirane) is an orally bioavailable small molecule with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) by inhibiting the phosphorylation of signal transducer and activator of transcription 3 (STAT3). Atiprimod also downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB transcription factors .
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-
- HY-123034
-
|
|
CDK
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CDKI-83 is a potent CDK9 and CDK1 inhibitor with Ki values of 21 nM and 72 nM for CDK9/T1 and CDK1/B, respectively. CDKI-83 demonstrates effective anti-proliferative activity in human tumour cell lines with a GI50<1 μM. CDKI-83 effectively induces apoptosis in A2780 human ovarian cancer cells. CDKI-83 reduces phosphorylation at Ser-2 of RNA polymerase II (RNAPII) by inhibiting cellular CDK9 activity, and down-regulates Mcl-1 and Bcl-2. CDKI-83 has the potential for anti-cancer research .
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-
- HY-15191B
-
|
(S)-BI-97C1
|
Bcl-2 Family
|
Cancer
|
|
(S)-Sabutoclax ((S)-BI-97C1), an optically pure apogossypol derivative, is pan-active inhibitor of antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. (S)-Sabutoclax (Compound II) inhibits the binding of BH3 peptides to Bcl-XL, Bcl-2, Mcl-1, and Bfl-1 with IC50 values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. (S)-Sabutoclax also potently inhibits cell growth of human prostate cancer, lung cancer, and lymphoma cell lines with EC50 values of 0.13, 0.56, and 0.049 μM, respectively. (S)-Sabutoclax can be used for the research of apoptosis-based therapies against cancer .
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-
- HY-162619
-
|
|
Apoptosis
CDK
|
Cancer
|
|
CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC50 values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity .
|
-
- HY-101778
-
|
EU-5346
|
Bcl-2 Family
|
Cancer
|
|
ML311 is a potent and selective inhibitor of the Mcl-1/Bim interaction.
|
-
- HY-122627
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CLZ-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. CLZ-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells .
|
-
- HY-N3913
-
|
|
STAT
Bcl-2 Family
|
Cancer
|
|
Furowanin A is a flavonoid with anti-neoplastic effects. Furowanin A inhibits STAT3/Mcl-1 axis to suppress proliferation, block cell cycle progression, induce apoptosis and promote autophagy. Furowanin A potently inhibits colorectal cancer (CRC) cells .
|
-
- HY-19471
-
|
|
Others
|
Cancer
|
|
(rac)-ZK-304709 is an isomer of ZK-304709. It is a first-in-class oral multi-target tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (Cdks), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. It directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. In an orthotopic BON tumor model, (rac)-ZK-304709 reduced primary tumor growth by 80% and reduced tumor microvascular density. These results suggest that (rac)-ZK-304709 can effectively control tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may be a potential agent for the treatment of NET.
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-
- HY-164466
-
|
|
Calcium Channel
Notch
|
Cancer
|
|
CAD204520, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL) .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-18628S
-
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|
|
UMI-77-d4 is the deuterium labeled UMI-77. 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 Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
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