2. Signaling Pathways
  3. Apoptosis
  4. Bcl-2 Family

Bcl-2 Family

Bcl-2 Family

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Bcl-2 is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). There are a total of 25 genes in the Bcl-2 family known to date. Human genes encoding proteins that belong to this family include: Bak1, Bax, Bal-2, Bok, Mcl-1.

Bcl-2 Family Isoform Specific Products:

Bcl-2 Family Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N4327
    Eurycomalactone
    		Inhibitor 98.99%
    Eurycomalactone is an active quassinoid could be isolated from Eurycoma longifolia Jack. Eurycomalactone is a potent NF-κB inhibitor with an IC50 value of 0.5 μM. Eurycomalactone inhibits protein synthesis and depletes cyclin D1. Eurycomalactone enhances radiosensitivity through arrest cell cycle at G2/M phase and delayed DNA double-strand break repair. Eurycomalactone inhibits the activation of AKT/NF-κB signaling, induces apoptosis and enhances chemosensitivity to Cisplatin (HY-17394).
    Eurycomalactone
  • HY-16232
    Glufosfamide
    		Inhibitor 98.0%
    Glufosfamide is a glucose-conjugated alkylating cytotoxic agent and a derivative of Ifosfamide (HY-17419). Glufosfamide induces apoptosis frequency and increase the expression of caspase-9 and caspase-3 in cancer cells. Glufosfamide shows great anti-tumor activity in MiaPaCa-2-RFP mouse model. Glufosfamide can be used for the study of hepatocellular carcinoma, prostate cancer and pancreatic carcinoma.
    Glufosfamide
  • HY-N2359
    Chelerythrine
    		Inhibitor
    Chelerythrine is a natural alkaloid, acts as a potent and selective Ca2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
    Chelerythrine
  • HY-134008
    Protoapigenone
    		Inducer 99.84%
    Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC50s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively.
    Protoapigenone
  • HY-RS08230
    MCL1 Human Pre-designed siRNA Set A
    		Inhibitor

    MCL1 Human Pre-designed siRNA Set A contains three designed siRNAs for MCL1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MCL1 Human Pre-designed siRNA Set A
  • HY-12826
    IMB-XH1
    		Inhibitor 98.0%
    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.
    IMB-XH1
  • HY-170380
    XY221
    		Inhibitor
    XY221 (Compound 16o) selectively inhibits BRD4 BD2, with an IC50 of 5.8 nM. XY221 demonstrates high pan-BD2 selectivity (667-fold over BRD4 BD1) and BRD4 BD2 domain selectivity (9−32-fold over BRD2/3/T BD2). XY221 induce Apoptosis in MV4-11 cells and shows anticancer activity .
    XY221
  • HY-101996
    SMBA1
    		Agonist
    SMBA1 is a potent Bax agonist with a Ki value of 43.3 nM. SMBA1 enhances the Bax expression. SMBA1 shows anti-tumor activity. SMBA1 has the potential for the research of lung cancer.
    SMBA1
  • HY-170406
    BCL-XL-IN-3
    		Inhibitor
    BCL-XL-IN-3 (Compound 11) is an inhibitor for BCL-XL with a Ki < 0.01 nM. BCL-XL-IN-3 inhibits the cell viability in normal Molt-4 and Digitonin (HY-N4000)-permeabilized Molt-4 with EC50 of 77.8 nM and 0.07 nM. BCL-XL-IN-3 can be used as ADC toxin for synthesis of Clezutoclax (HY-137774).
    BCL-XL-IN-3
  • HY-13408
    (+)-Apogossypol
    		Inhibitor
    (+)-Apogossypol is a pan-BCL-2 antagonist. (+)-Apogossypol binds to Mcl-1, Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 µM, respectively.
    (+)-Apogossypol
  • HY-N6651
    Isocryptotanshinone
    		Inhibitor ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC.
    Isocryptotanshinone
  • HY-147889
    BBR-BODIPY
    		Activator 98.15%
    BBR-BODIPY is a fluorescent probe that allows screening its interaction with the targeted cells. BBR-BODIPY induces apoptosis and changes the expression of apoptosis-related proteins.
    BBR-BODIPY
  • HY-N5033
    17-Hydroxy sprengerinin C
    		Activator 99.68%
    17-Hydroxy sprengerinin C (compound 10) is a glycoside compound isolated from rhizomes of Polygonatum sibiricum. 17-Hydroxy sprengerinin C possesses stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.
    17-Hydroxy sprengerinin C
  • HY-X0009A
    Tambiciclib dimaleate
    		Degrader
    Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research.
    Tambiciclib dimaleate
  • HY-N1904
    4′-Hydroxywogonin
    		Inhibitor 98.22%
    4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis.
    4′-Hydroxywogonin
  • HY-N0867
    13-Oxyingenol-13-dodecanoate
    		Inhibitor 99.37%
    13-Oxyingenol-dodecanoate (13OD) is a tumor suppressor agent. 13-Oxyingenol-dodecanoate has anti-HIV-1 activity with EC50 value of 33.7 nM.13-Oxyingenol-dodecanoate can induce the expression of ULK1 to effect mitochondrial dysfunction and cellular autophagy. 13-Oxyingenol-dodecanoate also increases the expression of BAX and suppresses the expression of BCL-2 to effect apoptosis.
    13-Oxyingenol-13-dodecanoate
  • HY-129159
    (-)-Clerosterol
    		99.80%
    (-)-Clerosterol is a natural product that can be isolated from Codium fragile.
    (-)-Clerosterol
  • HY-N9802
    n-Butyl-β-D-fructofuranoside
    		Activator
    n-Butyl-β-D-fructofuranoside could be isolated from kangaisan. n-Butyl-β-D-fructofuranoside induces apoptosis through the mitochondrial pathway. n-Butyl-β-D-fructofuranoside can be used for cancer research.
    n-Butyl-β-D-fructofuranoside
  • HY-129179B
    (Rac)-Lisaftoclax
    		Inhibitor 98.22%
    (Rac)-Lisaftoclax ((Rac)-APG-2575) is a Bcl-2 inhibitor that can be uesd for hematologic malignancy research (CN112898295A).
    (Rac)-Lisaftoclax
  • HY-14521B
    Lometrexol hydrate
    		Inducer 99.20%
    Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    Lometrexol hydrate
Cat. No. Product Name / Synonyms Application Reactivity
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Download Bcl-2 Family Signaling Pathway Map.

Bcl-2 family members have been grouped into three classes. The anti-apoptotic subfamily contains the Bcl-2, Bcl-XL, Bcl-w, Mcl-1, Bfl1/A-1, and Bcl-B proteins, which suppress apoptosis and contain all four Bcl-2 homology domains, designated BH1-4. The pro-apoptotic subfamily contain BH1-3 domains, such as Bax, Bak, and Bok. A third class of BH3 only proteins Bad, Bid, Bim, Noxa and Puma have a conserved BH3 domain that can bind and regulate the anti-apoptotic BCL-2 proteins to promote apoptosis [1].


The intrinsic pathway is initiated by various signals, principally extracellular stimuli. BH3-only proteins (Bim, Bid, Bad, Noxa, Puma) engage with anti-apoptotic Bcl-2 family proteins to relieve their inhibition of Bax and Bak to activate them. Next, Bax and Bak are oligomerized and activated, leading to mitochondrial outer membrane permeabilization. Once mitochondrial membranes are permeabilized, cytochrome c and/or Smac/DIABLO is released into the cytoplasm, wherein they combine with an adaptor molecule, Apaf-1, and an inactive initiator Caspase, Pro-caspase 9, within a multiprotein complex called the apoptosome. Smac/DIABLO inhibits IAPs to activate Caspase 9. Caspase 9 activates Caspase 3, which is the initiation step for the cascade of Caspase activation. The extrinsic pathway can be activated by cell surface receptors, such as Fas and TNF Receptor, subsequently activating Caspase 8, and leads to Caspase 3 activation and cell demolition. Caspases in turn cleave a series of substrates, activate DNases and orchestrate the demolition of the cell. Bcl-2 family proteins are also found on the endoplasmic reticulum and the perinuclear membrane in hematopoietic cells, but they are predominantly localized to mitochondria [2]. 

 

Reference:
[1]. Cotter TG, et al. Apoptosis and cancer: the genesis of a research field. Nat Rev Cancer. 2009 Jul;9(7):501-7.

[2]. Kang MH, et al. Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res. 2009 Feb 15;15(4):1126-32.

Bcl-2 Family Isoform Comparison

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