Search Result
Results for "
BCL-2 inhibitor
" in MedChemExpress (MCE) Product Catalog:
6
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-129179
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APG-2575; BCL-2/BCL-xl inhibitor 1
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Bcl-2 Family
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Cancer
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Lisaftoclax (compound 6) is a dual Bcl-2 and Bcl-xl inhibitor with anti-tumor activity, extracted from patent WO2018027097A1. Lisaftoclax exhibits IC50 values of 2 nM and 5.9 nM for Bcl-2 and Bcl-xl, respectively .
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-
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- HY-156877
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-
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- HY-143873
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Bcl-2 Family
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Cancer
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Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155) .
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- HY-149623
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Bcl-2 Family
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Cancer
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Bcl-2-IN-13 is a Bcl-2 inhibitor with an IC50 value of 17 nM. Bcl-2-IN-13 can be used in cancer research .
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-
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- HY-149624
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Others
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Cancer
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Bcl-2-IN-14 (Compound 13c) is a BCL-2 inhibitor with an IC50 value of 0.471 μM. Bcl-2-IN-14 can be used in cancer research .
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- HY-163308
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Bcl-2 Family
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Cancer
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Bcl-2-IN-18 (Compound 23) is a breast cancer Bcl-2 inhibitor with a IC50 value of 4.7 μM for MCF-7. Bcl-2-IN-18 has antitumor activity .
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-
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- HY-129179B
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(Rac)-APG-2575
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Bcl-2 Family
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Cancer
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(Rac)-Lisaftoclax ((Rac)-APG-2575) is a Bcl-2 inhibitor that can be uesd for hematologic malignancy research (CN112898295A) .
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-
-
- HY-149009
-
|
Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells .
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- HY-143872
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Bcl-2 Family
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Cancer
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Bcl-2-IN-4 is a potent, orally active and selective Bcl-2 inhibitor with an IC50 of 1.5 nM. Bcl-2-IN-4 displays >200-fold selectivity over Bcl-xL (IC50 of 411 nM). Bcl-2-IN-4 inhibits RS4; 11 cell proliferation with an IC50 of 2.7 nM (WO2021180040A1; compound 2) .
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-
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- HY-149681
-
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Bcl-2 Family
Beclin1
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Cancer
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Beclin1-Bcl-2 interaction inhibitor 1 potently inhibits Beclin 1/Bcl-2 binding. Beclin1-Bcl-2 interaction inhibitor 1 can be used for the research of cancer and neurodegeneration .
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-
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- HY-135273
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BCL2-IN-1
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Bcl-2 Family
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Cancer
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A-1211212 (BCL2-IN-1) is a potent Bcl-2 inhibitor. BCL2-IN-1 binds Bcl-2 with a Ki of <0.01 nM .
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- HY-118874
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Bcl-2 Family
Apoptosis
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Cancer
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Oblimersen is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen can be used for cancer research .
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- HY-118874A
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Apoptosis
Bcl-2 Family
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Cancer
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Oblimersen sodium is a BCL-2 inhibitor targeting BCL-2 RNA. Oblimersen sodium specifically binds to the first six codons of the bcl-2 mRNA sequence, resulting in degradation of bcl-2 mRNA and induces apoptosis by down-regulating expression of Bcl-2. Oblimersen sodium can be used for cancer research .
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- HY-10087
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ABT-263
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Bcl-2 Family
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Cancer
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Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM .
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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-131247
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Bcl-2 Family
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Inflammation/Immunology
Cancer
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Bcl-2-IN-2 is a potent and selective Bcl-2 inhibitor with an IC50 of 0.034 nM and also inhibits Bcl-xL with an IC50 of 43 nM, showing >1000-fold selectivity for Bcl-2 over Bcl-xL .
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- HY-10087S
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Bcl-2 Family
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Cancer
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Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].
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-
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- HY-156620
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-
-
- HY-149436
-
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CDK
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Cancer
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CDK2/Bcl2-IN-1 (compound 1), a saponin and a CDK-2 inhibitor (IC50=117.6 nM) with promising cytotoxicity against cancer cells. CDK2/Bcl2-IN-1 also inhibits Bcl-2, and induces apoptosis in A549 lung cancer cells .
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- HY-163309
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Bcl-2 Family
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Cancer
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Bcl-2-IN-19 (compound 27) is a potent Bcl-2 inhibitor for targeting breast cancer .
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- HY-142209
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-
-
- HY-12011
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HA14-1
1 Publications Verification
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Bcl-2 Family
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Cancer
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HA14-1 is a Bcl-2/Bcl-XL antagonist. HA14-1 binds the designated pocket on Bcl-2 with the IC50 of ≈9 μM in competing with the Bcl-2 binding of Flu-BakBH3, and inhibits its function.
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- HY-149622
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Bcl-2 Family
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Cancer
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Bcl-2-IN-12 (Compound 1) is a Bcl-2 inhibitor (IC50: 6 nM). Bcl-2-IN-12 can be used for cancer research .
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- HY-149625
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Bcl-2 Family
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Cancer
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Bcl-2-IN-15 (Compound 13d)) is a Bcl-2 inhibitor (IC50: 363 nM). Bcl-2-IN-15 inhibits the proliferation ofNCI leukemia cancer cell line .
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- HY-160108
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Bcl-2 Family
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Others
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Bcl-2-IN-17 is a Bcl2 inhibitor and can be used for the research of diseases associated with Bcl anti-apoptotic protein .
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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-19551
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ApoG2
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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-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-153953
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Bcl-2 Family
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Cancer
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Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia .
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- HY-16014
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Bcl-2 Family
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Cancer
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A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
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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-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-N8579
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Others
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Inflammation/Immunology
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Eugenyl benzoate has the potency for scavenging of DPPH radical. Eugenyl Benzoate Derivatives can be used for development of BCL-2 inhibitors .
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- HY-50868
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INNO-406; NS-187
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Bcr-Abl
Src
Apoptosis
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Cancer
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Bafetinib is an orally active Lyn/Bcr-Abl tyrosine kinase inhibitor. Bafetinib enhances the activity of several pro-apoptotic Bcl-2 homology (BH) 3-pure proteins (Bim, Bad, Bmf, and Bik) through intrinsic apoptotic pathways regulated by the Bcl-2 family, and induces apoptosis of Ph + leukemia cells. Bafetinib has antitumor activity .
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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-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-144792
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Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
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Cancer
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Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
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- HY-144791
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Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
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Cancer
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Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
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- HY-18106
-
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Bcl-2 Family
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Cancer
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BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM 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-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-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-N1218
-
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Stellasterol is a natural product. Stellasterol has high affinity towards Bcl-2 protein (Ki: 118.05 nM). Stellasterol is a weak α-glucosidase inhibitor .
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-
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- HY-N2897
-
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Apoptosis
Bcl-2 Family
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Inflammation/Immunology
|
Dihydrokaempferol is isolated from Bauhinia championii (Benth). Dihydrokaempferol induces apoptosis and inhibits Bcl-2 and Bcl-xL expression. Dihydrokaempferol is a good candidate for new antiarthritic agents .
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-
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- HY-100762
-
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Bcl-2 Family
|
Cancer
|
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-120882
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UBX1967
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Bcl-2 Family
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Cancer
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BM-1197 (UBX1967) is a potent and selective inhibitor of dual Bcl-2/Bcl-xL, with IC50s of 3.5 nM and 5.2 nM for Bcl-2 and Bcl-xL, respectively. BM-1197 exhibits antitumor effects both in vitro and in vivo .
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- HY-15531
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Venetoclax
Maximum Cited Publications
123 Publications Verification
ABT-199; GDC-0199; RG7601
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Bcl-2 Family
Autophagy
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Cancer
|
Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy .
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- HY-117288
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S55746
1 Publications Verification
BCL201
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Bcl-2 Family
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Cancer
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S55746 (BCL201) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 (BCL201) has antitumor activity with low toxicity .
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- HY-133772
-
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Drug Metabolite
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Others
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Venetoclax N-oxide is an impurity of Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM .
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- HY-117288A
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BCL201 hydrochloride
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Bcl-2 Family
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Cancer
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S55746 hydrochloride (BCL201 hydrochloride) is a potent, orally active and selective BCL-2 inhibitor, with a Ki of 1.3 nM and a Kd of 3.9 nM. S55746 hydrochloride (BCL201 hydrochloride) has antitumor activity with low toxicity .
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- HY-119931
-
-
- HY-150540
-
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Bcl-2 Family
Apoptosis
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Cancer
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Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research .
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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-138832
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APG-1252-M1
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Bcl-2 Family
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Cancer
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BM-1244 (APG-1252-M1) is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively. BM-1244 inhibits senescent fibroblasts (SnCs) with an EC50 of 5 nM. (From patent WO2019033119A1) .
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- HY-N3828
-
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Apoptosis
ERK
JNK
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Cancer
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epi-Eriocalyxin A (Epieriocalyxin A), a diterpenoid isolated from Isodon eriocalyx, induces colon cancer apoptosis. epi-Eriocalyxin A also inhibits ERK1/2 and JNK activation, which suppresses Bcl-2 expression .
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- HY-161254
-
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Apoptosis
MDM-2/p53
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Inflammation/Immunology
|
ATPase-IN-3 (compound 6) is a ATPase inhibitor. ATPase-IN-3 has Gastroprotective effect in ethanol-induced gastric ulcers by contribution of anti-apoptotic (BCL-2) and tumor suppressor (P53) proteins .
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- HY-130604
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DT2216
1 Publications Verification
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Bcl-2 Family
PROTACs
Apoptosis
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Cancer
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DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax (HY-10087), a linker, and a VHL E3 ubiquitin ligase (Red: Navitoclax; Blue: VHL ligand; Black: linker) .
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- HY-10969
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GX15-070 Mesylate
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Bcl-2 Family
Autophagy
Parasite
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Infection
Cancer
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Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
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- HY-10969A
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GX15-070
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Bcl-2 Family
Autophagy
Parasite
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Infection
Cancer
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Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
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- HY-148026
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BGB 11417
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Bcl-2 Family
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Cancer
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Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines .
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- HY-112416
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AZD4320
1 Publications Verification
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Bcl-2 Family
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Cancer
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AZD4320 is a novel BH3-mimicking dual BCL2/BCLxL inhibitor with IC50s of 26 nM, 17 nM, and 170 nM for KPUM-MS3, KPUM-UH1, and STR-428 cells, respectively.
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- HY-15531S
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ABT-199-d8; GDC-0199-d8; RG7601-d8
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Bcl-2 Family
Autophagy
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Cancer
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Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
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- HY-118119
-
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PGE synthase
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Cancer
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CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
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- HY-P1733
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BMF-Y
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Apoptosis
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Cancer
|
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
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- HY-13846
-
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Bcl-2 Family
Apoptosis
|
Cancer
|
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM .
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- HY-50907
-
|
Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
|
Cancer
|
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
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- HY-109184
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AMG 397
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Bcl-2 Family
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Cancer
|
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-121934
-
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Others
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Cancer
|
BH3I-2' is the BH3I-2 analogue. BH3I-2 is a Bcl-2 family inhibitor. BH3I-2' can be used for various studies .
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- HY-15191B
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(S)-BI-97C1
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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 .
|
-
- HY-18628
-
UMI-77
1 Publications Verification
|
Bcl-2 Family
|
Cancer
|
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.
|
-
- HY-N2741
-
|
Bcl-2 Family
|
Cancer
|
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
|
-
- HY-50907S
-
|
Biochemical Assay Reagents
|
Cancer
|
ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-100383
-
BHI1; BH 3I1
|
Bcl-2 Family
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
|
-
- HY-N0087
-
Beta-Guttiferrin
|
Bcl-2 Family
Autophagy
|
Cancer
|
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.
|
-
- HY-146097
-
|
P-glycoprotein
Apoptosis
|
Cancer
|
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 .
|
-
- HY-18628S
-
|
Isotope-Labeled Compounds
Bcl-2 Family
|
Cancer
|
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.
|
-
- HY-115974
-
|
Others
|
Cancer
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis. Anticancer activity .
|
-
- HY-146817
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-11 is a potent tubulin polymerization inhibitor with an IC50 value of 3.4 µM. Tubulin polymerization-IN-11 shows antiproliferative activity. Tubulin polymerization-IN-11 induces Apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-11 decreases the expression of cyclin B1, p-cdc2, and Bcl-2 protein levels and increases the expression of cleaved PARP .
|
-
- HY-155242
-
|
VEGFR
Bcl-2 Family
Apoptosis
|
Cancer
|
VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM) .
|
-
- HY-123823
-
NCX 4016
|
COX
Apoptosis
|
Cancer
|
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins .
|
-
- HY-N0292
-
|
Cytochrome P450
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
|
-
- HY-107738
-
Z/E-Guggulsterone
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
Cancer
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
|
-
- HY-146253
-
|
CDK
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
|
-
- HY-111329
-
ILS-JGB-1741
|
Sirtuin
Apoptosis
|
Cancer
|
JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
|
-
- HY-156096
-
|
HDAC
Histone Methyltransferase
Caspase
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels .
|
-
- HY-157176
-
|
Others
|
Others
|
BAX-IN-1 is a potential, selective inhibitor of Bcl-2-associated X protein (BAX).
|
-
- HY-109185
-
APG-1252
|
Bcl-2 Family
Apoptosis
|
Cancer
|
Pelcitoclax (APG-1252) is a potent Bcl-2/Bcl-xl inhibitor with antineoplastic and pro-apoptotic effects .
|
-
- HY-161100
-
|
Apoptosis
|
Cancer
|
BDM19 binds and activates cytosolic BAX dimers, and prompts cell apoptosis either alone or in combination with BCL-2/BCL-XL inhibitor Navitoclax (HY-10087) .
|
-
- HY-162148
-
|
EGFR
|
Cancer
|
HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
|
-
- HY-155188
-
|
Bcl-2 Family
|
Neurological Disease
|
NWP-0476 is BCL-2/BCL-xL inhibitor. NWP-0476 has a modified structure with fine-tuned BCL-xL activity. NWP-0476 can be used for relapsed T-acute lymphoblastic leukemia (T-ALL) research .
|
-
- HY-143235
-
|
Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
|
Cancer
|
BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
|
-
- HY-156278
-
|
Apoptosis
Autophagy
|
Cancer
|
FB49 is a highly selective inhibitor of Bcl-2-associated athanogene 3 (BAG3), with the Ki of 45 μM. FB49 inhibits the cell growth in human tumoral cells, but has no toxicity in human peripheral mononuclear cells. FB49 block cell cycle in G1 phase and to induce apoptosis as well as autophagy in medulloblastoma HD-MB03 treated cells .
|
-
- HY-144778
-
|
Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
|
Cancer
|
IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
|
-
- HY-N0265
-
|
Caspase
Apoptosis
|
Cardiovascular Disease
|
Asperosaponin VI, A saponin component from Dipsacus asper, induces osteoblast differentiation through BMP‐2/p38 and ERK1/2 pathway . Asperosaponin Ⅵ inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB .
|
-
- HY-103271
-
|
Bcl-2 Family
|
Cancer
|
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
|
-
- HY-B0011
-
RP-56976
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
|
-
- HY-151428
-
|
Ferroptosis
Apoptosis
Bcl-2 Family
COX
|
Cancer
|
Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
|
-
- HY-151429
-
|
Apoptosis
Ferroptosis
Bcl-2 Family
COX
|
Cancer
|
Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
|
-
- HY-B0011A
-
RP-56976 Trihydrate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM . Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis .
|
-
- HY-B0011S
-
RP-56976-d9
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
|
-
- HY-B0011R
-
RP-56976 (Standard)
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
Docetaxel (Standard) is the analytical standard of Docetaxel. This product is intended for research and analytical applications. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
|
-
- HY-B0011AS
-
RP-56976-d5 trihydrate
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
|
-
- HY-151443
-
|
HDAC
|
Cancer
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-150596
-
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-147826
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1733
-
BMF-Y
|
Apoptosis
|
Cancer
|
BMf-BH3 (BMF-Y) belongs to the Bcl-2 apoptosis mediator family. BH3-only protein, Bmf is a key molecule for histone deacetylase (HDAC) inhibitors mediated enhancing effect on ionizing radiation-induced cell death .
|
-
- HY-103271
-
|
Bcl-2 Family
|
Cancer
|
Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N2897
-
-
-
- HY-119931
-
-
-
- HY-149436
-
-
-
- HY-N8579
-
-
-
- HY-N3828
-
-
-
- HY-N2741
-
-
-
- HY-N0087
-
-
-
- HY-N0292
-
-
-
- HY-107738
-
Z/E-Guggulsterone
|
Triterpenes
Structural Classification
Classification of Application Fields
Terpenoids
Plants
Burseraceae
Disease Research Fields
Commiphora wightii
Cancer
|
Apoptosis
JNK
Akt
Caspase
FXR
Autophagy
|
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
|
-
-
- HY-N0265
-
-
-
- HY-B0011
-
-
-
- HY-B0011R
-
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10087S
-
|
Navitoclax-d8 is the deuterium labeled Navitoclax. Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM[1].
|
-
-
- HY-50907S
-
|
ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
-
- HY-B0011S
-
|
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
|
-
-
- HY-15531S
-
|
Venetoclax-d8 is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy[1][2][3].
|
-
-
- HY-18628S
-
|
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.
|
-
-
- HY-B0011AS
-
|
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
|
-
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