1. Signaling Pathways
  2. Apoptosis
  3. Apoptosis

Apoptosis

Apoptosis

Apoptosis is a distinctive form of cell death exhibiting specific morphological and biochemical characteristics, including cell membrane blebbing, chromatin condensation, genomic DNA fragmentation, and exposure of specific phagocytosis signaling molecules on the cell surface. Cells undergoing apoptosis differ from those dying through necrosis. Necrotic cells are usually recognized by the immune system as a danger signal and, thus, resulting in inflammation; in contrast, apoptotic death is quiet and orderly.

There are two major pathways of apoptotic cell death induction: The intrinsic pathway, also called the Bcl-2-regulated or mitochondrial pathway, is activated by various developmental cues or cytotoxic insults, such as viral infection, DNA damage and growth-factor deprivation, and is strictly controlled by the BCL-2 family of proteins. The extrinsic or death-receptor pathway is triggered by ligation of death receptors (members of the tumor necrosis factor (TNF) receptor family, such as Fas or TNF receptor-1 (TNFR1)) that contain an intracellular death domain, which can recruit and activate caspase-8 through the adaptor protein Fas-associated death domain (FADD; also known as MORT1) at the cell surface. This recruitment causes subsequent activation of downstream (effector) caspases, such as caspase-3, -6 or -7, without any involvement of the BCL-2 family.

Studies suggest that alterations in cell survival contribute to the pathogenesis of a number of human diseases, including cancer, viral infections, autoimmune diseases, neurodegenerative disorders, and AIDS (acquired immunodeficiency syndrome). Treatments designed to specifically alter the apoptotic threshold may have the potential to change the natural progression of some of these diseases.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108713A
    Famitinib malate
    Inducer
    Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer.
    Famitinib malate
  • HY-137433A
    Befotertinib mesylate
    Inducer
    Befotertinib (D-0316) mesylate is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib mesylate selectively targets EGFR mutations including EGFRT790M, EGFRL858R and delE746-A750, forms covalent bonds with EGFRC797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib mesylate inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib mesylate can be used in research related to multidrug-resistant cancers and non-small cell lung cancer.
    Befotertinib mesylate
  • HY-B0425R
    Novobiocin (Standard)
    Inducer
    Novobiocin (Standard) is the analytical standard of Novobiocin. This product is intended for research and analytical applications. Novobiocin (Albamycin) is a potent and orally active antibiotic. Novobiocin also is a DNA gyrase inhibitor and a heat shock protein 90 (Hsp90) antagonist. Novobiocin has the potential for the research of highly beta-lactam-resistant pneumococcal infections. Novobiocin shows anti-orthopoxvirus activity.
    Novobiocin (Standard)
  • HY-181050
    DFCI-002-06
    Inducer
    DFCI-002-06 is an orally active dual-target HCK/BTK PROTAC degrader with DC₅₀ values for HCK and BTK of 1.3 and 4.5 nM respectively. DFCI-002-06 retains higher anti-tumor activity than the HCK/BTK dual-target inhibitor (HY-15805), inducing apoptosis in cancer cells. DFCI-002-06 can be used for the study of MYD88 mutant B-cell malignancies.
    DFCI-002-06
  • HY-B0580C
    Ketorolac hemicalcium
    Inducer 98.06%
    Ketorolac (RS37619) hemicalcium is a non-steroidal anti-inflammatory drug (NSAID), acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. Ketorolac tromethamine is used as 0.5% ophthalmic solution for the research of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and postoperative ocular inflammation and pain. Ketorola chemicalcium is also a DDX3 inhibitor that can be used for cancer research.
    Ketorolac hemicalcium
  • HY-B0256A
    Azathioprine sodium
    Inducer
    Azathioprine (BW 57-322) sodium is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis.
    Azathioprine sodium
  • HY-B1041AS
    Aminoguanidine-13C, 15N4
    Aminoguanidine-13C,15N4 (Pimagedine-13C,15N4) is the 13C- and 15N-labeled Aminoguanidine (HY-B1041A). Aminoguanidine (Pimagedine hydrochloride) is an inhibitor of diamine oxidase and nitric oxide synthase. Aminoguanidine has a dose-dependent inhibitory effect on apoptosis induced by Doxorubicin (HY-15142). Aminoguanidine has antioxidant properties. Aminoguanidine can be used in diabetic nephropathy research.
    Aminoguanidine-13C, 15N4
  • HY-W011303R
    Phytosphingosine (Standard)
    Inducer
    Phytosphingosine (Standard) is the analytical standard of Phytosphingosine. This product is intended for research and analytical applications. Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes[1][2][3][4].
    Phytosphingosine (Standard)
  • HY-13502B
    Mitoxantrone diacetate
    Inducer
    Mitoxantrone diacetate is a potent topoisomerase II inhibitor. Mitoxantrone diacetate also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone diacetate induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone diacetate shows antitumor activity. Mitoxantrone diacetate also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.
    Mitoxantrone diacetate
  • HY-183623
    ProAlk01
    Inducer
    ProAlk01 is a protein alkylating agent that serves as a toxin payload for ADCs. ProAlk01 localizes to the cytoplasm and exerts cytotoxic effects mainly by alkylating cytoplasmic proteins rather than binding to DNA. ProAlk01 induces cell cycle arrest, apoptosis, and immunogenic cell death. ProAlk01 can be used in the research of solid tumors.
    ProAlk01
  • HY-112852A
    TL02-59 dihydrochloride
    Activator
    TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth.
    TL02-59 dihydrochloride
  • HY-138059A
    SM-433 hydrochloride
    Inducer 98.57%
    SM-433 hydrochlorid, a Smac mimetic, function as inhibitor of inhibitor of apoptosis proteins (IAPs). SM-433 hydrochlorid exhibits strong binding affinity XIAP BIR3 protein with an IC50<1 μM (patent WO2008128171A2).
    SM-433 hydrochloride
  • HY-111277
    CEP-14513
    Inducer
    CEP-14513 is an ALK inhibitor with an IC50 of 4 nM. CEP-14513 also inhibits insulin receptor, VEGFR2, TIE2 and DLK kinases, but does not inhibit MET, IKKβ, or CDK1/2/5. CEP-14513 induces cancer cell apoptosis. CEP-14513 is applicable to research related to non-small cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroblastic tumor, and diffuse large B-cell lymphoma.
    CEP-14513
  • HY-B0349B
    Meclizine dihydrochloride monohydrate
    Modulator
    Meclizine (Meclozine) dihydrochloride monohydrate, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride monohydrate is an effective anti-motion sickness agent. Meclizine dihydrochloride monohydrate crosses the blood-brain barrier. Meclizine dihydrochloride monohydrate is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine dihydrochloride monohydrate can be used for the research of polyQ toxicity disorders, such as Huntington's disease.
    Meclizine dihydrochloride monohydrate
  • HY-151207
    Anticancer agent 81
    Inducer
    Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab.
    Anticancer agent 81
  • HY-16168B
    Degarelix acetate hydrate
    Inducer
    Degarelix acetate hydrate (FE 200486 acetate hydrate) is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR/LHRHR) antagonist. Degarelix acetate hydrate can be used for prostate cancer research.
    Degarelix acetate hydrate
  • HY-146096
    RMS3
    Inducer
    RMS3, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS3 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS3 has strong anticancer property.
    RMS3
  • HY-145736A
    β-Glucuronide-dPBD-PEG5-NH2 TFA
    Inducer
    β-Glucuronide-dPBD-PEG5-NH2 TFA is the β-glucuronide-linked pyrrolobenzodiazepine dimer, which binds to the prenylated antibody for synthesis of antibody-drug conjugate (ADC) cIRCR201-dPBD.β-glucuronide-linkage as a cleavable linker. β-Glucuronide-dPBD-PEG5-NH2 TFA, as a proagent of cIRCR201-dPBD, reduces side effects. β-Glucuronide-dPBD-PEG5-NH2 TFA can induce apoptosis and arrest cell cycle. β-Glucuronide-dPBD-PEG5-NH2 TFA has antitumor activity.
    β-Glucuronide-dPBD-PEG5-NH2 TFA
  • HY-146097
    RMS5
    Inducer
    RMS5, a tetrandrine analogue, is a potent P-glycoprotein (P-gp) inhibitor. RMS5 has markedly antiproliferative and cytotoxic effects on cancer cells. RMS5 slightly diminishes the expression of the anti-apoptotic Bcl-2 family proteins Bcl-XL and Mcl-1. RMS3 causes PARP cleavage, a marker for cells undergoing apoptosis. RMS5 has strong anticancer property.
    RMS5
  • HY-12018A
    Vatalanib hydrochloride
    Inhibitor
    Vatalanib (PTK787; ZK-222584; CGP-797870) hydrochloride is a BBB-permeable VEGFR2/KDR inhibitor with an IC50 of 37 nM.
    Vatalanib hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity