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

Bcl-2 Family

Bcl-2 Family

Related Products

PDF 0.66 MB

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-175175
    MAPK-IN-5
    		Inhibitor
    MAPK-IN-5 is a potent MAPK inhibitor with an IC50 of 1.35 μM against HeLa cells. MAPK-IN-5 inhibits HeLa cell proliferation by inducing ROS-mediated DNA damage and mitochondrial apoptosis via the MAPK pathway. MAPK-IN-5 significantly inhibits colony formation, reduces the number of live cells, suppresses cell migration, and causes cell cycle arrest in the G2/M phase in HeLa cells. MAPK-IN-5 can be used for the study of cervical cancer.
    MAPK-IN-5
  • HY-181836
    IKKβ-IN-6
    		Modulator
    IKKβ-IN-6 is an antitumor agent. IKKβ-IN-6 inhibits IKKβ (IC50: 18.24 μM), thereby suppressing the phosphorylation of p65 and IκBα, blocking the nuclear translocation of p65, and subsequently regulating genes controlled by NF-κB. IKKβ-IN-6 also targets topoisomerase I (Topo I), induces DNA damage, ROS accumulation, loss of mitochondrial membrane potential, and S-phase arrest. IKKβ-IN-6 is applicable to related research on colorectal cancer.
    IKKβ-IN-6
  • HY-181769
    Anticancer agent 306
    		Modulator
    Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer.
    Anticancer agent 306
  • HY-179615
    Entadamide A-CO-C12
    		Modulator
    Entadamide A-CO-C12 is an Entadamide A (HY-N12125) derivative with potent anti-cancer activity, particularly against breast cancer cell lines. Entadamide A-CO-C12 promotes apoptosis, suppresses migratory ability, sphere formation, and stem-like cell populations. Entadamide A-CO-C12 inhibits tumor growth in a 4T1 mouse model. Entadamide A-CO-C12 can be used for the research of breast cancer.
    Entadamide A-CO-C12
  • HY-115718B
    PZ703b hydrochloride
    		Degrader 99.18%
    PZ703b hydrochloride is a Bcl-xl PROTAC degrader that induces apoptosis and inhibits cancer cell proliferation. PZ703b hydrochloride can be used for the research of bladder cancer research.
    PZ703b hydrochloride
  • HY-182349
    Bax activator-2
    		Activator
    Bax activator-2 is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μM against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, cleavage of caspase-3/9 and PARP, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against a variety of cancer cell lines. Bax activator-2 can be used in research related to acute myeloid leukemia and solid tumors.
    Bax activator-2
  • HY-13407S
    Gossypol-13C2
    Gossypol-13C2 (BL 193-13C2) is an active compound. Gossypol-13C2 can be used for kinds of research.
    Gossypol-<sup>13</sup>C<sub>2</sub>
  • HY-175397
    Dth
    		Inhibitor
    Dth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research.
    Dth
  • HY-181795
    CSN5-IN-3
    		Inhibitor
    CSN5-IN-3 (Compound 30) is a CSN5 inhibitor with an IC50 of 0.58 μM. CSN5-IN-3 inhibits the enzymatic activity of CSN5, leading to increased accumulation of NEDD8-Cul1 and promoting the degradation of PD-L1. CSN5-IN-3 downregulates Bcl-2, and upregulates P53 and Cleaved caspase-3. CSN5-IN-3 exhibits anticancer activity against triple-negative breast cancer.
    CSN5-IN-3
  • HY-178036
    ZM484
    		Inhibitor
    ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
    ZM484
  • HY-170912
    Topo I/II-IN-2
    Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
    Topo I/II-IN-2
  • HY-169124
    Apoptosis inducer 28
    		Inhibitor
    Apoptosis Inducer 28 (Compound X1) is an apoptosis-inducing agent with anticancer activity in vitro. Apoptosis Inducer 28 can arrest the cell cycle at the G1 phase, promote cell death, and induce apoptosis by disrupting mitochondrial membrane potential. Apoptosis inducer 28 can also decrease the production of reactive oxygen species, downregulate the gene expression of BAX, Bcl-xL, and Bcl-2, while upregulating the gene expression of PAR-4.
    Apoptosis inducer 28
  • HY-136893
    SP-6-27
    		Activator
    SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer.
    SP-6-27
  • HY-W743417
    (-)-Norgestrel-d6
    (-)-Norgestrel-d6 is the deuterium labeled Levonorgestrel (HY-B0257). Levonorgestrel is an orally active inhibitor of progesterone (HY-N0437). Levonorgestrel has anticancer activity and can induce Apoptosis. Levonorgestrel can be used as a contraceptive and in combination with other medications. Levonorgestrel can be used in the study of osteoporosis and uterine leiomyoma.
    (-)-Norgestrel-d<sub>6</sub>
  • HY-114118F5
    Semaglutide, Cy5 labeled
    Semaglutide, Cy5 labeled is a CY5 (HY-D0821) labeled Semaglutide (HY-114118), which is suitable for high-sensitivity fluorescence detection and imaging (Ex/Em = 633/670 nm).
    Semaglutide, Cy5 labeled
  • HY-169267
    BRD-K44839765
    		Inhibitor
    BRD-K44839765 is selective against Bcl-2 with an IC50 value of 5.6 μM in IMR-90 cell. BRD-K44839765 has oral activity.
    BRD-K44839765
  • HY-180190
    Tubulin polymerization-IN-85
    Tubulin polymerization-IN-85 (Compound C21) is a tubulin polymerization inhibitor (IC50 = 1.59 μM) targeting the colchicine binding site. Tubulin polymerization-IN-85 can cause cancer cells G2/M phase arrest and induce apoptosis. Tubulin polymerization-IN-85 downregulates the expression of Bcl-2, Bcl-xl, Mcl-1, Cyclin B1, cdc25, cdc2 protein and upregulates P53, P21, Bad and Bax levels. Tubulin polymerization-IN-85 can be used for the research of cancer, such as cervical cancer.
    Tubulin polymerization-IN-85
  • HY-RS01423
    Bcl2l1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Bcl2l1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Bcl2l1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Bcl2l1 Rat Pre-designed siRNA Set A
  • HY-179614
    PARP1-IN-50
    PARP1-IN-50 is a selective and orally active PARP-1 inhibitor with an IC50 of 64.98 nM. PARP1-IN-50 can inhibit PAR formation and induce DNA double strand breaks, thereby causing DNA damage. PARP1-IN-50 can induce G2/M phase arrest and cancer cells apoptosis. PARP1-IN-50 demonstrates significant antiproliferative activity against various cancer cells. PARP1-IN-50 can be used for the research of cancer, such as breast cancer.
    PARP1-IN-50
  • HY-182031
    JS04
    		Activator
    JS04 is a EGFRL858R/T790M kinase inhibitor. JS04 activates both endogenous and exogenous apoptosis (apoptosis) pathways and induces G2/M phase arrest of the cell cycle. JS04 is applicable to the research of drug-resistant non-small cell lung cancer.
    JS04
Cat. No. Product Name / Synonyms Application Reactivity
All Rights Reserved.
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

Your Search Returned No Results.

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

Please try each isoform separately.