Bcl-2
Bcl-2 (B-cell lymphoma 2) is a central anti-apoptotic regulator that preserves mitochondrial integrity by preventing mitochondrial outer membrane permeabilization (MOMP), a critical checkpoint controlling cytochrome c release and caspase activation during intrinsic apoptosis[1][2]. Mechanistically, Bcl-2 functions through direct interactions with pro-apoptotic BCL-2 family proteins, including Bax and Bak, thereby suppressing their oligomerization and limiting mitochondrial membrane disruption[3][4]. The protein also integrates signals transmitted by BH3-only proteins, which regulate the balance between cell survival and programmed cell death under physiological and pathological stress conditions[3][5]. Dysregulated Bcl-2 expression contributes to apoptosis resistance in multiple malignancies and supports tumor cell survival by maintaining mitochondrial homeostasis despite cellular stress[6][7]. In disease models, the anti-apoptotic activity of Bcl-2 is closely linked to mitochondrial apoptosis pathways that represent major therapeutic targets in hematologic and solid cancers[6][8]. Compared with related anti-apoptotic isoforms such as Mcl-1 and Bcl-B, Bcl-2 displays broader interactions with both Bax and Bak, whereas Mcl-1 and Bcl-B show preferential regulation of Bak- and Bax-dependent apoptotic pathways, respectively[4]. For experimental applications, BH3-mimetic inhibitors disrupt the interaction between Bcl-2 and pro-apoptotic partners, thereby restoring mitochondrial apoptosis and providing a widely used strategy for mechanistic studies and targeted cancer research[7][8].
References:
- [1]. Harris MH, et al. The role of the Bcl-2 family in the regulation of outer mitochondrial membrane permeability. Cell Death Differ. 2000;7:1182-1191.
- [2]. Breckenridge DG, et al. Regulation of mitochondrial membrane permeabilization by BCL-2 family proteins and caspases. Curr Opin Cell Biol. 2004;16(6):647-652.
- [3]. Kale J, et al. BCL-2 family proteins: changing partners in the dance towards death. Cell Death Differ. 2018;25:65-80.
- [4]. Zhai D, et al. Differential regulation of Bax and Bak by anti-apoptotic Bcl-2 family proteins Bcl-B and Mcl-1. J Biol Chem. 2008 Apr 11;283(15):9580-6. [Content Brief]
- [5]. Lomonosova E, et al. BH3-only proteins in apoptosis and beyond: an overview. Oncogene. 2008 Dec;27 Suppl 1(Suppl 1):S2-19. [Content Brief]
- [6]. Danial NN. BCL-2 family proteins: critical checkpoints of apoptotic cell death. Clin Cancer Res. 2007;13(24):7254-7263.
- [7]. Akl H, et al. A dual role for the anti-apoptotic Bcl-2 protein in cancer: Mitochondria versus endoplasmic reticulum. Biochim Biophys Acta. 2014;1843(10):2240-2252.
- [8]. Kang MH, et al. Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res. 2009 Feb 15;15(4):1126-32. [Content Brief]
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Bcl-2 Related Products (283)
Related Products (283)
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Antibodies (6)
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Venetoclax
0 ImagesSynonyms: ABT-199; GDC-0199; RG7601
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Sorafenib
0 ImagesSynonyms: Bay 43-9006Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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Polyinosinic-polycytidylic acid
0 ImagesSynonyms: Poly(I:C)Polyinosinic-polycytidylic acid (Poly(I:C)) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid can directly trigger cancer cells to undergo apoptosis.
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Navitoclax
0 ImagesSynonyms: ABT-263Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM.
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ABT-737
0 ImagesABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.
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MS1 peptide
0 ImagesMS-1 peptide is a peptide for BH3 profiling. MS-1 peptide triggers higher depolarization of mitochondrial membrane in melanoma cells pre-treated with Encorafenib (HY-15605). MS1 peptide can be used for the research of BRAFV600E melanoma.
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CMIT/MIT (2.0-2.5% in water)
0 ImagesCat. No.: HY-W017982ACAS No.: 55965-84-9Synonyms: CMI/MI (2.0-2.5% in water)CMIT/MIT (2.0-2.5% in water) (CMI/MI (2.0-2.5% in water)) is a mixture of CMIT and MIT, and is also a preservative and skin sensitizer. CMIT/MIT (2.0-2.5% in water) increases the levels of phosphorylated ERK1/2, p38, JNK1/2, p53, p21 and Bax, decreases the level of Bcl-2, and activates the Nrf-2/HO-1 signaling pathway. CMIT/MIT (2.0-2.5% in water) increases LDH release and lipid peroxidation levels, impairs antioxidant defense capacity, promotes pro-inflammatory cytokine release, induces apoptosis, triggers cell cycle arrest, exhibits neurotoxicity in neuroblastoma cells, and causes dysregulation of Th2/Th17 immune responses. CMIT/MIT (2.0-2.5% in water) can be used in studies related to allergy, atopic dermatitis and lung injury.
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Bcl-2-IN-25
0 ImagesCat. No.: HY-184107CAS No.: 2290611-27-5
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Beta-Sitosterol (purity>98%)
0 ImagesSynonyms: β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc.
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Lonafarnib
0 ImagesSynonyms: Sch66336Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria.
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Sorafenib tosylate
0 ImagesSynonyms: Bay 43-9006 tosylateSorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma.
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MRT68921
0 ImagesMRT68921 is a potent NUAK1/ULK1 dual inhibitor. MRT68921 inhibits ULK1 and ULK2 with IC50 values of 2.9 nM and 1.1 nM, respectively. MRT68921 can block cells autophagy and kill tumor cells by breaking the balance of oxidative stress signals. MRT68921 can inhibit cell proliferation and induce ROS production and apoptosis. MRT68921 can be used for the research of cancer, such as breast cancer.
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A-1155463
0 ImagesA-1155463, a chemical probe, is a highly potent and selective BCL-XL inhibitor with an EC50 of 70 nM in Molt-4 cell. A-1155463 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Digitoxin
0 ImagesDigitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
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Amantadine
0 ImagesAmantadine (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.
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Poly (I:C):Kanamycin (1:1)
0 ImagesCat. No.: HY-107202APoly(I:C):Kanamycin (1:1) is a mixture of Poly(I:C) (HY-107202) and Kanamycin (HY-16566). Poly(I:C) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Poly(I:C) can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Poly(I:C) can directly trigger cancer cells to undergo apoptosis. Kanamycin stabilizes Poly(I:C).
