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-143872
    Bcl-2-IN-4
    		Inhibitor
    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).
    Bcl-2-IN-4
  • HY-169412
    MAPK-IN-3
    		Inhibitor
    MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK.
    MAPK-IN-3
  • HY-169083
    Bcl-2-IN-22
    		Inhibitor
    Bcl-2-IN-22 (compound 1) is a gold(I) NHC complex with anticancer activity. Bcl-2-IN-22 induces apoptosis via the mitochondrial pathway with an IC50 value of 0.014 μM. In addition, Bcl-2-IN-22 targets BCL-2 family members and exhibits pro-apoptosis and resensitization properties in multidrug-resistant leukemia cells that overexpress BCL?2.
    Bcl-2-IN-22
  • HY-RS01418
    BCL2A1 Human Pre-designed siRNA Set A
    		Inhibitor

    BCL2A1 Human Pre-designed siRNA Set A contains three designed siRNAs for BCL2A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    BCL2A1 Human Pre-designed siRNA Set A
    BCL2A1 Human Pre-designed siRNA Set A
  • HY-148281
    TMX-2164
    		Inhibitor
    TMX-2164 is a potent, irreversible B-cell lymphoma 6 (BCL6) inhibitor with an IC50 value of 152 nM. TMX-2164 displays sustained target engagement and antiproliferative activity in cells.
    TMX-2164
  • HY-117652
    Lobetyol
    		Modulator
    Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Lobetyol
  • HY-123034
    CDKI-83
    		Inhibitor
    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.
    CDKI-83
  • HY-129702
    MCL-1/BCL-2-IN-4
    		Inhibitor
    MCL-1/BCL-2-IN-4 (Compound 7) is a potent and selective Mcl-1 and Bcl-2 dual inhibitor.
    MCL-1/BCL-2-IN-4
  • HY-138071
    8α-Tigloyloxyhirsutinolide 13-O-acetate
    		Inhibitor
    8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.
    8α-Tigloyloxyhirsutinolide 13-O-acetate
  • HY-153096A
    OICR12694 TFA
    		Inhibitor
    OICR12694 (JNJ-65234637) TFA is an orally active inhibitor of B cell lymphoma 6 (BCL6).
    OICR12694 TFA
  • HY-163681
    Zamzetoclax
    		Inhibitor
    Zamzetoclax (compound 1) is a potential Mcl-1 inhibitor.
    Zamzetoclax
  • HY-132997
    PROTAC Bcl-xL degrader-3
    		Inhibitor
    PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader (WO2020163823A2, compound 44).
    PROTAC Bcl-xL degrader-3
  • HY-B0402S1
    Amantadine-d6
    		98.10%
    Amantadine-d6 is the deuterium labeled Amantadine[1]. Amantadine (1-Adamantanamine) is an orally avtive and potent antiviral agent with activity against influenza A viruses. Amantadine inhibits several ion channels such as NMDA and M2, and also inhibits Coronavirus ion channels. Amantadine also has anti-orthopoxvirus and anticancer activity. Amantadine can be used for Parkinson's disease, postoperative cognitive dysfunction (POCD) and COVID-19 research[2][3][4][5][6][7].
    Amantadine-d<sub>6</sub>
  • HY-155245
    A09-003
    		Inhibitor
    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.
    A09-003
  • HY-P2012
    TRP-601
    TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia.
    TRP-601
  • HY-170689
    CG-3-246
    		Inhibitor
    CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research.
    CG-3-246
  • HY-116204
    SKLB70326
    		Inhibitor
    SKLB70326 is a small molecule inhibitor of cell cycle progression, which has the activity of inducing G?/G? phase arrest and apoptosis in human hepatoma cells. SKLB70326 can inhibit the proliferation of human hepatoma cells, induce cell cycle arrest and apoptosis, and its mechanism is related to downregulating cyclin-dependent kinase (CDK) 2, CDK4 and CDK6, while activating PARP, caspase-3, caspase-9 and Bax, and downregulating Bcl-2.
    SKLB70326
  • HY-163293
    Mcl-1 inhibitor 18
    		Inhibitor
    Mcl-1 inhibitor 18 (compound 57) is a myeloid cell leukemia 1 (Mcl-1) inhibitor, and can be used for study of cancer.
    Mcl-1 inhibitor 18
  • HY-W689801
    A-1208746
    		Inhibitor
    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.
    A-1208746
  • HY-123020
    CYD-2-88
    		Antagonist
    CYD-2-88 (BDA-366 analog) is a BDA-366 (HY-101083) (Bcl2 BH4 antagonist) analog. CYD-2-88 (20 mg/kg, i.p.) inhibits tumor growth in NSCLC H460 xenografts mice.
    CYD-2-88
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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