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

Bcl-2 Family

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-159817
    Asaretoclax
    Inhibitor
    Asaretoclax is a potent B-cell lymphoma 2 (Bcl-2) inhibitor. Asaretoclax has the potential for the research of cancer.
    Asaretoclax
  • HY-122721
    Mcl1-IN-5
    Inhibitor
    Mcl1-IN-5 (compound 21) is a MCL-1 inhibitor. Mcl1-IN-5 can be used for the research of cancers.
    Mcl1-IN-5
  • HY-150540
    Bcl-2-IN-10
    Inhibitor
    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.
    Bcl-2-IN-10
  • HY-167825
    Barakol
    Barakol is a major compound found in Cassia siamea. Barakol inhibits MMP-3 activity. Barakol potentiates the anti-metastatic effect of Doxorubicin (HY-15142). Barakol induces apoptosis, with ROS generation, increase in expression ratio of Bax/Bcl-2, and caspase-9 activation. Barakol has laxative, anxiolytic, CNS depressant, and antioxidant, anticancer effects.
    Barakol
  • HY-RS01417
    BCL2 Rat Pre-designed siRNA Set A
    Inhibitor

    BCL2 Rat Pre-designed siRNA Set A contains three designed siRNAs for BCL2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    BCL2 Rat Pre-designed siRNA Set A
    BCL2 Rat Pre-designed siRNA Set A
  • HY-RS01359
    Bak1 Rat Pre-designed siRNA Set A
    Inhibitor

    Bak1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bak1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Bak1 Rat Pre-designed siRNA Set A
    Bak1 Rat Pre-designed siRNA Set A
  • HY-RS01426
    Bcl2l10 Rat Pre-designed siRNA Set A
    Inhibitor

    Bcl2l10 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bcl2l10 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Bcl2l10 Rat Pre-designed siRNA Set A
    Bcl2l10 Rat Pre-designed siRNA Set A
  • HY-146184
    CCT373567
    Inhibitor
    CCT373567 is a potent molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.9 nM. CCT373567 exhibits antiproliferative activity.
    CCT373567
  • HY-176219
    Bcl-2-IN-23
    Inhibitor
    Bcl-2-IN-23 (compound 5) is a selective inhibitor targeting Bcl-2. The IC50 of Bcl-2-IN-23 in HTB-140, HeLa and SW620 cells is 25.7-33.7 μM. Bcl-2-IN-23 can non-covalently competitively bind to Bcl-2 protein, significantly reduce its expression, and induce late apoptosis and necroptosis of cancer cells. Bcl-2-IN-23 enhances the sensitivity of cancer cells to apoptosis and reduces the release of IL-6 inflammatory factors by disrupting the Bcl-2-mediated mitochondrial apoptosis inhibition pathway. Bcl-2-IN-23 can be used for anti-apoptosis research of malignant tumors such as melanoma, cervical cancer, and colorectal cancer.
    Bcl-2-IN-23
  • HY-151429
    Antitumor agent-77
    Inhibitor
    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.
    Antitumor agent-77
  • 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-123564
    Mcl1-IN-7
    Inhibitor
    Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.
    Mcl1-IN-7
  • 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-168877
    FMP
    FMP is a Platinum(IV) complexe. FMP significantly upregulates the expression of γ-H2AX and p53. FMP increases the production of ROS. FMP markedly upregulates the expressions of Apoptosis-related proteins (DR5, Fas, caspase-8, Cyt-c, caspase-3, cleaved-PARP1, Bax). FMP shows antiproliferative activity against breast cancer.
    FMP
  • HY-RS01357
    BAK1 Human Pre-designed siRNA Set A
    Inhibitor

    BAK1 Human Pre-designed siRNA Set A contains three designed siRNAs for BAK1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    BAK1 Human Pre-designed siRNA Set A
    BAK1 Human Pre-designed siRNA Set A
  • 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
Cat. No. Product Name / Synonyms Application Reactivity

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.

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.