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-144428
    Bcl-2/Mcl-1-IN-2
    		Inhibitor
    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.
    Bcl-2/Mcl-1-IN-2
  • HY-169266
    BRD-K56819078
    		Inhibitor
    BRD-K56819078 is a Bcl-2 inhibitor that significantly reduces senescent cell load and senescence-related genes in the kidney mRNA expression. BRD-K56819078 exerts anti-aging effects by inhibiting apoptosis.
    BRD-K56819078
  • HY-143235
    BRD4 Inhibitor-15
    		Modulator
    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.
    BRD4 Inhibitor-15
  • HY-169265
    BRD-K20733377
    		Inhibitor
    BRD-K20733377 is an inhibitor for Bcl-2, and exhibits selective cytotoxicity against senescent cells, that inhibits the viability of Etoposide (HY-13629)-induced IMR-90 senescent cell with an IC50 of 10.7 μM. BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21 and KI67 in aged mouse model.
    BRD-K20733377
  • HY-162642
    Bfl-1-IN-3
    		Inhibitor
    Bfl-1-IN-3 (Compound 56) is a selective, competitive inhibitor for Bfl-1 on BID binding site with Ki of 105 nM. Bfl-1-IN-3 inhibits the proliferation of cell pfeiffer and MV4-11, with IC50 of 6.92 μM and 12.6 μM. Bfl-1-IN-3 induces apoptosis in pfeiffer cells. Bfl-1-IN-3 overcomes Venetoclax (HY-15531) resistance at the cellular level, and shows synergistically enhanced anti-tumor activity with Venetoclax.
    Bfl-1-IN-3
  • HY-159588
    Mcl-1 inhibitor 20
    		Inhibitor
    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.
    Mcl-1 inhibitor 20
  • HY-146038
    Antitumor agent-55
    		Inhibitor
    Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3.
    Antitumor agent-55
  • HY-150266
    A-1293102
    		Inhibitor
    A-1293102 is a potent and selective BCL-XL inhibitor that kills BCL-XL-dependent tumor cells.
    A-1293102
  • HY-151428
    Antitumor agent-78
    		Inhibitor
    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.
    Antitumor agent-78
  • HY-150507
    JNJ-4355
    		Inhibitor
    JNJ-4355 is a highly potent MCL-1 (myeloid cell leukemia-1) inhibitor, with KI of 18 pM. JNJ-4355 shows antitumor activity.
    JNJ-4355
  • HY-P5324
    Bad BH3 (mouse)
    Bad BH3 (mouse) is a biological active peptide. (This is a bcl-2 binding peptide. This peptide is derived from the BH3 domain (a death domain) of Bad, amino acid residues 140 to 165.)
    Bad BH3 (mouse)
  • HY-149522
    WK499
    		Inhibitor
    BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC50s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively).
    WK499
  • HY-100866A
    F1324 TFA
    		Inhibitor
    F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
    F1324 TFA
  • HY-N1218
    Stellasterol
    Stellasterol is a natural product. Stellasterol has high affinity towards Bcl-2 protein (Ki: 118.05 nM). Stellasterol is a weak α-glucosidase inhibitor.
    Stellasterol
  • HY-154962
    Mcl-1 inhibitor 15
    		Inhibitor
    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.
    Mcl-1 inhibitor 15
  • HY-161874
    RPS6-IN-1
    		Inducer
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-148899
    Mcl-1 inhibitor 10
    		Inhibitor
    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.
    Mcl-1 inhibitor 10
  • HY-10087A1
    Navitoclax dihydrochloride
    		Inhibitor
    Navitoclax (ABT-263) dihydrochloride is an orally active Bcl-2 inhibitor that binds to various Bcl-2 family proteins, including Bcl-xL, Bcl-2, and Bcl-w, with a Ki value of less than 1 nM. Navitoclax dihydrochloride can be used in cancer research.
    Navitoclax dihydrochloride
  • HY-17495
    Carteolol
    		Activator
    Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research.
    Carteolol
  • HY-N6626R
    Pyraclostrobin (Standard)
    Pyraclostrobin (Standard) is the analytical standard of Pyraclostrobin. This product is intended for research and analytical applications. Pyraclostrobin is a highly effective and broad-spectrum strobilurin fungicide. Pyraclostrobin can induce oxidative DNA damage, mitochondrial dysfunction and autophagy through the activation of AMPK/mTOR signaling. Pyraclostrobin can be used to control crop diseases.
    Pyraclostrobin (Standard)
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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