Bcl-2 Family
Bcl-2 family proteins are a group of proteins homologous to the Bcl-2 protein and characterized by containing at least one of four conserved Bcl-2 homology (BH) domains (BH1, BH2, BH3 and BH4). Bcl-2 family proteins, consisting of pro-apoptotic and anti-apoptotic molecules, can be classified into the following three subfamilies according to sequence homology within four BH domains: (1) a subfamily shares sequence homology within all four BH domains, such as Bcl-2, Bcl-XL and Bcl-w which are anti-apoptotic; (2) a subfamily shares sequence homology within BH1, BH2 and BH4, such as Bax and Bak which are pro-apoptotic; (3) a subfamily shares sequence homology only within BH3, such as Bik and Bid which are pro-apoptotic.
Products for Bcl-2 Family
- Cat.No. Product Name Information
- GC17008 (+)-Apogossypol inhibitor of Bcl-2 family proteins
- GC34980 (E)-Ferulic acid (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299.
- GC34096 (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) (R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
- GC35001 (S)-Gossypol acetic acid (S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
- GC12258 2,3-DCPE hydrochloride
- GC17512 A-1155463 BCL-XL inhibitor, potent and selective
- GC16278 A-1210477 MCL-1 inhibitor
- GC17513 A-1331852 BCL-XL inhibitor, potent and selective
- GC32981 A-385358 A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
- GC64674 ABBV-167 ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.
- GC14069 ABT-199 A Bcl-2 inhibitor
- GC12405 ABT-263 (Navitoclax) ABT-263 (Navitoclax) is a inhibitor of Bcl-xL, Bcl-2 and Bcl-w, with Ki ≤0.5 nM, ≤1 nM and ≤1 nM respectively.
- GC17234 ABT-737 An inhibitor of anti-apoptotic Bcl-2 proteins
- GN10341 Acetate gossypol
- GC19452 AMG-176 AMG-176 (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM.
- GC14080 Apogossypolone (ApoG2)
- GC11106 AT-101
- GC33247 AZD-5991 An Mcl-1 inhibitor
- GC33283 AZD-5991 Racemate 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.
- GC33239 AZD-5991 S-enantiomer 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.
- GC33255 AZD4320 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.
- GC34263 Bak BH3 Bak BH3 is derived from the BH3 domain of Bak, can antagonize the function of Bcl-xL in cells.
- GC12053 BAM7 A direct activator of Bax
- GC12763 Bax channel blocker
- GC16023 Bax inhibitor peptide P5 Bax inhibitor
- GC17195 Bax inhibitor peptide V5 A Bax inhibitor
- GC16695 Bax inhibitor peptide, negative control Peptide inhibit Bax translocation to mitochondria
- GC63325 Bcl-xL antagonist 2 Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-XL with an IC50 and Ki of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).
- GC62599 BCL6-IN-4 BCL6-IN-4 is a potent B-cell lymphoma 6 (BCL6) inhibitor with an IC50 of 97 nM. BCL6-IN-4 has anti-tumor activities.
- GC68012 BCL6-IN-7
- GC10721 BDA-366 BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells.
- GC18136 BH3I-1 Bcl-2 or Bcl-XL inhibitor
-
GC15987
BIM, Biotinylated
Bim peptide fragment with a biotin moiety attached
- GC33407 BM 957 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.
- GC13498 BM-1074
- GC62871 BM-1244 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).
- GC38014 BT2 An Mcl-1 inhibitor
- GC31806 Bz 423 (BZ48) Bz 423 (BZ48) is a pro-apoptotic 1,4-benzodiazepine with therapeutic properties in murine models of lupus demonstrating selectivity for autoreactive lymphocytes, and activates Bax and Bak.
- GC62561 CCT369260 CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC50 of 520 nM.
- GN10463 Chelerythrine
- GC13065 Chelerythrine Chloride Potent inhibitor of PKC and Bcl-xL
- GN10219 Ciwujianoside-B
- GC60111 Clitocine Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity.
- GN10040 Dehydrocorydaline
- GC10661 Destruxin B insecticidal and phytotoxic activity;induces apoptosis
- GC38617 Dihydrokaempferol A flavone with diverse biological activities
- GC35882 dMCL1-2 dMCL1-2 is a potent and selective PROTAC of myeloid cell leukemia 1 (MCL1) (Bcl-2 family member) based on Cereblon, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1.
- GC12139 Gambogic Acid A xanthonoid with anticancer activity
- GC32998 Ginsenoside Rh4
- GC34134 Glycocholic acid A glycine-conjugated form of cholic acid
- GN10082 Gossypol
- GC11510 HA14-1 A Bcl-2 inhibitor
- GC12046 iMAC2
- GN10645 Jaceosidin
- GC64467 Lisaftoclax 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.
- GC15480 Marinopyrrole A Marinopyrrole A (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).
- GC66017 Mcl-1 inhibitor 6 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.
- GC38927 MCL-1/BCL-2-IN-2 MCL-1/BCL-2-IN-2 (Compound 6) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
- GC38928 MCL-1/BCL-2-IN-3 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.
- GC36556 Mcl1-IN-1 Mcl1-IN-1 is an inhibitor of myeloid cell factor 1 (Mcl-1) (IC50=2.4 ?M).
- GC36557 Mcl1-IN-11 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.
- GC36558 Mcl1-IN-12 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.
- GC33035 Mcl1-IN-2 Mcl1-IN-2 is an inhibitor of myeloid cell factor 1 (Mcl-1). Mcl1-IN-2 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of Mcl1-IN-2 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.
- GC33347 Mcl1-IN-3 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.
- GC33364 Mcl1-IN-4 Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.
- GC38811 Mcl1-IN-8 Mcl1-IN-8 (Compound 8) is an orally active Mcl-1-PUMA interface inhibitor, with a Ki of 0.3 μM. Mcl1-IN-8 exhibits dual activity on reduce PUMA-dependent apoptosis while deactivating Mcl-1-mediated anti-apoptosis in cancer cells.
- GC36559 Mcl1-IN-9 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.
- GC33295 MIK665 (S-64315) MIK665 (S-64315) (S-64315), derived from S63845, is a myeloid cell leukemia sequence 1 (MCL1) inhibitor. MIK665 (S-64315) has an IC50 of 1.81 nM for MCL1.
- GC15400 MIM1 An Mcl-1 inhibiting molecule
- GC33312 ML311 An Mcl-1 inhibitor
- GC61096 MSN-125 MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity.
- GC63083 MSN-50 MSN-50 is a Bax and Bak oligomerization inhibitor.
- GC16938 Muristerone A An ecdysteroid receptor agonist
- GC62707 Murizatoclax 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.
- GC68019 NPB
- GC25673 Obatoclax (GX15-070)
- GC11569 Obatoclax mesylate (GX15-070) An antagonist of pro-survival Bcl-2 proteins
- GC36855 Paris saponin VII Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
- GC62505 Pelcitoclax Pelcitoclax (APG-1252) is a potent Bcl-2/Bcl-xl inhibitor with antineoplastic and pro-apoptotic effects.
- GC63769 PROTAC Bcl-xL degrader-2 PROTAC Bcl-xL degrader-2 is a potent Bcl-xL (Bcl-2 family member) degrader based on von Hippel-Lindau ligand, with an IC50 of 0.6 nM.
- GC38941 PROTAC Bcl2 degrader-1 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.
- GC38943 PROTAC Mcl1 degrader-1 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 induces the ubiquitination and proteasomal degradation of Mcl-1 by introducing the E3 ligase cereblon (CRBN)-binding ligand pomalidomide to Mcl-1 inhibitor S1-6 with μM-range affinity.
- GC34389 PUMA BH3 PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.
- GC12902 Pyridoclax Mcl-1 inhibitor
- GC11140 Radotinib(IY-5511) Bcr-Abl tyrosine kinase inhibitor
- GC32947 S55746 (BLC201) S55746 (BLC201) (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 (BLC201) (BCL201) has antitumor activity with low toxicity.
- GC33401 S55746 hydrochloride (BLC201 (hydrochloride)) S55746 hydrochloride (BLC201 (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 (BLC201 (hydrochloride)) (BCL201 hydrochloride) has antitumor activity with low toxicity.
- GC12621 S63845 MCL1 inhibitor
- GC62554 S65487 S65487 (VOB560), a potent and selective BCL-2 inhibitor, is a prodrug 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.
- GC63426 S65487 hydrochloride S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is a prodrug 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.
- GC63531 S65487 sulfate S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, is a prodrug 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.
- GC10153 Sabutoclax A pan-Bcl-2 inhibitor
- GC10567 TCPOBOP constitutive androstane receptor (CAR) agonist
- GC37780 Thevetiaflavone Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.
- GC66021 TP-021 TP-021 (BCL6-IN-8c) is a potent and orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 μM in cell-free enzyme-linked immunosorbent assay.
- GC12649 TW-37 An inhibitor of the Bcl-2 family proteins
- GC15805 UMI-77 Mcl-1 inhibitor, novel
-
GC70114
Venetoclax-d8
Venetoclax-d8 is the deuterated form of Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly efficient, selective and orally effective Bcl-2 inhibitor with a Ki value less than 0.01 nM. Venetoclax can induce autophagy.
- GC33052 VU0661013 VU661013 is a potent and selective MCL-1 inhibitor.
- GC11921 WEHI-539 A selective Bcl-xL inhibitor