2. Signaling Pathways
  3. Apoptosis
  4. Apoptosis

Apoptosis

Apoptosis

Apoptosis

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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-181726
    BRAFV600E/ABL2-IN-2
    		Inducer
    BRAFV600E/ABL2-IN-2 is a dual BRAFV600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma.
    BRAFV600E/ABL2-IN-2
  • HY-171509
    Mal-N(Me)-C6-N(Me)-PNU-159682
    		Inducer
    Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).
    Mal-N(Me)-C6-N(Me)-PNU-159682
  • HY-180159
    Tubulin-IN-63
    		Inducer
    Tubulin-IN-63 is a potent tubulin polymerization inhibitor targeting the colchicine-binding site, with an IC50 of 6.03 µM. Tubulin-IN-63 disrupts microtubule dynamics, induces G2/M arrest and apoptosis, thereby suppressing cancer cell proliferation. Tubulin-IN-63 disrupts capillary network formation in human umbilical vein endothelial cells (HUVECs) and exhibits in vivo antitumor efficacy in a B16-F10 mouse model. Tubulin-IN-63 can be used for the research of cancers, such as melanoma, lung cancer, and liver cancer.
    Tubulin-IN-63
  • HY-181763
    Tubulin-IN-65
    		Inducer
    Tubulin-IN-65 (Compound Imp-18) is a Tubulin inhibitor. Tubulin-IN-65 exhibits tubulin-disrupting activity. Tubulin-IN-65 disrupts microtubule integrity. Tubulin-IN-65 induces Apoptosis and increases the expression of CDK1 and Cyclin B1. Tubulin-IN-65 possesses anticancer activity against breast cancer and colorectal cancer. Tubulin-IN-65 can be used in research related to triple-negative breast cancer and colorectal adenocarcinoma.
    Tubulin-IN-65
  • HY-P10614
    Bid BH3 peptide
    Bid BH3 peptide is a small peptide derived from Bid protein that can bind and activate the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and apoptosis. Bid BH3 peptide can be used to study mitochondrial bioenergetics.
    Bid BH3 peptide
  • HY-180618
    p53 DUBTAC modulator-1
    		Inducer
    p53 DUBTAC modulator-1 (Compound A1) is a p53 Y220C DUBTAC modulator (Kd = 12.09 µM). p53 DUBTAC modulator-1 effectively reactivates and deubiquitinates mutant p53 Y220C. p53 DUBTAC modulator-1 upregulates p53 Y220C protein levels. p53 DUBTAC modulator-1 induces Apoptosis, reduces Bcl-2, inhibits Wnt signaling. p53 DUBTAC modulator-1 has anti-cancer activity against liver cancer.
    p53 DUBTAC modulator-1
  • HY-N6777R
    Penicillic acid (Standard)
    		Inhibitor
    Tetracaine (hydrochloride) (Standard) is the analytical standard of Tetracaine (hydrochloride). This product is intended for research and analytical applications. Tetracaine hydrochloride (Amethocaine hydrochloride) is a calcium channel protein inhibitor and blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. Tetracaine hydrochloride is mainly used topically in ophthalmology and as an antipruritic.
    Penicillic acid (Standard)
  • HY-175299
    Hedgehog IN-11
    		Inducer
    Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM).
    Hedgehog IN-11
  • HY-165606
    SB-T-1214
    		Inducer
    SB-T-1214 (SBT) is a taxane. SB-T-1214 efficiently inhibits expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induces apoptosis of colon cancer spheroids with drug resistant tumorigenic CD133+/CD44+ cells. SB-T-1214 strongly represses tumor growth in Pgp+ DLD-1 human colon tumor xenografts mice model. SB-T-1214 can be used for antitumor research, especially against tumors with drug resistance, such as colon, pancreatic and renal cancers.
    SB-T-1214
  • HY-B0617B
    S-Adenosyl-L-methionine 1,4-butanedisulfonate
    		Inhibitor
    S-Adenosyl-L-methionine (S-Adenosyl methionine) 1,4-butanedisulfonate is an orally active methyl group donor. S-Adenosyl-L-methionine 1,4-butanedisulfonate is a dietary supplement with potent antidepressant effects. S-Adenosyl-L-methionine 1,4-butanedisulfonate also has anti‑proliferative, pro‑apoptotic and anti‑metastatic roles in cancers. S-Adenosyl-L-methionine 1,4-butanedisulfonate has the potential for, cancer, liver disease and osteoarthritis research.
    S-Adenosyl-L-methionine 1,4-butanedisulfonate
  • HY-182284
    Anticancer agent 310
    		Inducer
    Anticancer agent 310 is an antitumor agent. Anticancer agent 310 releases nitric oxide to induce mitochondrial ROS burst, triggers mitochondrial dysfunction and activates the Bax/Bcl-2-Cyt c-Caspase-9/Caspase-3 apoptotic pathway. Anticancer agent 310 also reduces the levels of SHMT2 and MTHFD2, decreases the ratios of NADPH/NADP+ and GSH/GSSG, thereby disrupting redox homeostasis and exacerbating intracellular ROS accumulation. Anticancer agent 310 can be used in research related to gastric cancer.
    Anticancer agent 310
  • HY-W744064
    Diethylstilbestrol-d4
    Diethylstilbestrol-d4 is the deuterium labeled Diethylstilbestrol (HY-14598). Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and?Apoptosis?of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte?Autophagy?Diethylstilbestrol is a?11β-hydroxysteroid dehydrogenase 2 (HSD11B2)?inhibitor.
    Diethylstilbestrol-d<sub>4</sub>
  • HY-113853
    WF-10129
    		Inducer
    WF-10129 is a cytotoxic steroidal compound isolated from the plant Physalis. WF-10129 inhibits liver cancer cell proliferation, induces apoptosis, interferes with metabolism, and significantly reduces lactate production in vitro and in vivo. WF-10129 can also exert anti-tumor activity by regulating the expression of related genes and proteins through the AKT-p53 pathway.
    WF-10129
  • HY-147825
    EGFR/BRAFV600E-IN-1
    		Activator
    EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.
    EGFR/BRAFV600E-IN-1
  • HY-126929
    Trioxacarcin B
    		Inducer
    Trioxacarcin B (TXN-B) is a potent cytotoxic agent and DNA-targeted inhibitor. Trioxacarcin B disrupts DNA function and induces apoptosis in cancer cells. Trioxacarcin B not only effectively inhibits the growth of various Gram-positive and Gram-negative bacteria as well as Plasmodium falciparum, but also blocks the colony formation of cancer stem cells, significantly reduces tumor volume and prolongs survival in preclinical in vivo models. The activity of Trioxacarcin B is highly dependent on its intact spiro-epoxide structure; it loses efficacy once this moiety undergoes hydrolysis, and Trioxacarcin B shows no activity against fungi, microalgae and small RNA viruses. Trioxacarcin B can be used for research on bacterial infections, malaria, and various cancers including colon cancer and melanoma.
    Trioxacarcin B
  • HY-145844
    EGFR-IN-44
    		Inducer
    EGFR-IN-44 (Compound 6a) is a potent, orally active EGFR tyrosine kinase inhibitor with an IC50 of 4.11 nM. EGFR-IN-44 induces cell apoptosis and shows an oral bioavailability value of 33.57%. EGFR-IN-44 can be studied for non-small-cell lung cancers.
    EGFR-IN-44
  • HY-W965550
    Apoptosis inducer 40
    		Inducer
    Apoptosis inducer 40 is an apoptosis inducer. Apoptosis inducer 40 exhibits potent cytotoxic effects against jurkat and NB4 cells with IC50 values of 4.5 μM and 3.6μM. Apoptosis inducer 40 induces apoptosis and arrests cell cycle. Apoptosis inducer 40 can be used for the research of cancer, such as acute myeloid leukemia (AML).
    Apoptosis inducer 40
  • HY-176171
    Tubulin polymerization-IN-79
    		Inducer
    Tubulin polymerization-IN-79 (Compound C20) is a tubulin polymerization inhibitor. Tubulin polymerization-IN-79 shows potent antiproliferative activity against esophageal cancer cells (e.g., KYSE450, IC50=0.36 μM; EC-109, IC50=0.63 μM). Tubulin polymerization-IN-79 occupies the colchicine binding site to disrupt microtubule network integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP expression, and inducing G2/M phase arrest and apoptosis in esophageal cancer cells. Tubulin polymerization-IN-79 is promising for research of esophageal cancers.
    Tubulin polymerization-IN-79
  • HY-173165
    OA-Br-1
    		Inducer
    OA-Br-1 is an orally active and selective inhibitor of PTP1B with an IC50 value of 7.08 μM. OA-Br-1 induces apoptosis. OA-Br-1 has broad spectrum anti-proliferative activity against cancer cells, and plays an anti-breast cancer role through the PTP1B/PI3K/AKT signaling pathway both in vitro and in vivo.
    OA-Br-1
  • HY-170323
    4-TM.P
    		Inducer
    4-TM.P binds to the minor groove of DNA, inhibits proliferation of cancer cell K562 with an IC50 of 25 µM, arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell K562. 4-TM.P can be used in anti-leukemia research.
    4-TM.P
Cat. No. Product Name / Synonyms Application Reactivity