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-183338
    SphK2-IN-4
    Inducer
    SphK2-IN-4 is a selective SphK2 inhibitor (IC50=6.2 μM) with extremely low activity against SphK1 (IC50 > 50 μM). SphK2-IN-4 exhibits broad-spectrum antiproliferative activity against colorectal cancer cells and induces apoptosis.
    SphK2-IN-4
  • HY-179451
    Apoptosis inducer 53
    Inducer
    Apoptosis inducer 53 is an apoptosis inducer. Apoptosis inducer 53 can inhibit proliferation of human tumor cell lines (A549, HeLa, SW1573, T-47D, WiDr) with GI50 values of 2.5-9.1 μM. Apoptosis inducer 53 can induce cancer cells apoptosis and reduce colony formation. Apoptosis inducer 53 can activate p38α MAPK signaling and exerts anti-inflammatory effect. Apoptosis inducer 53 also shows anti-Leishmania donovani activity. Apoptosis inducer 53 can be used for the researches of cancer, infection and inflammation.
    Apoptosis inducer 53
  • HY-145861
    LSD1-IN-14
    Inducer
    LSD1-IN-14 is a potent and selective LSD1 inhibitor (IC50=0.89 μM). LSD1-IN-14 can significantly inhibit the proliferation of A549 and THP-1 cells and induce the apoptosis of tumor cells.
    LSD1-IN-14
  • HY-173500
    MG-3C
    Inducer
    MG-3C is a potent matrix metalloproteinase 9 (MMP-9) inhibitor. MG-3C can selectively kill non-small-cell lung cancer (NSCLC) cells harboring the EGFR T790M mutation. MG-3C blocks the EGFR/STAT3 signaling pathway, inducing G2/M phase arrest, growth inhibition, and apoptosis of cancer cells. MG-3C is promising for research of lung cancer.
    MG-3C
  • HY-N11479
    Vallesiachotamine
    Inducer
    Vallesiachotamine, a known monoterpene indole alkaloid, possesses anti-tumor activity.
    Vallesiachotamine
  • HY-118823
    Amonafide L-malate
    Inducer
    Amonafide L-malate is a topoisomerase II inhibitor and DNA intercalator that induces Apoptotic signaling by blocking the binding of Topo II to DNA.
    Amonafide L-malate
  • HY-180850
    ERB-2
    Inducer
    ERB-2 is a selective ERβ PROTAC degrader. ERB-2 removes the inhibitory effect of ERβ on ROS, leading to the accumulation of ROS, mitochondrial damage, and ultimately triggering cell apoptosis (apoptosis). ERB-2 significantly inhibits tumor growth in the nude mouse model of NCI-H1975OR tumors. ERB-2 can be used for the study of non-small cell lung cancer.
    ERB-2
  • HY-146461
    Anticancer agent 58
    Inducer
    Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model.
    Anticancer agent 58
  • HY-155124
    Antiproliferative agent-32
    Inducer
    Antiproliferative agent-32 (Compound 1c) inhibits the phosphorylation of PI3K/Akt/mTOR signaling pathway. Antiproliferative agent-32 inhibits Huh7 and SK-Hep-1 cells proliferation, and induce cells apoptosis, causes mitochondrial damage. Antiproliferative agent-32 can be used for research of hepatocellular carcinoma.
    Antiproliferative agent-32
  • HY-146103
    Antiproliferative agent-7
    Inducer
    Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis.
    Antiproliferative agent-7
  • HY-173007
    ALK/PI3K/AKT-IN-1
    Inducer
    ALK/PI3K/AKT-IN-1 (Compound 45) inhibits the proliferation of cancer cell A549, H1975 and PC9 with an IC50 of 0.44, 0.83 and 1.51 μM. ALK/PI3K/AKT-IN-1 increases the expression of p21 and p27, inhibits the activity of CDK2 and p-Rb, arrests the cell cycle at G1 phase. ALK/PI3K/AKT-IN-1 inhibits the ALK/PI3K/AKT signaling pathway, promotes the depolarization of mitochondrial membrane potential, and inducing apoptosis in A549 cell. ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheroids.
    ALK/PI3K/AKT-IN-1
  • HY-175565
    Tubulin/VEGFR-2-IN-1
    Inducer
    Tubulin/VEGFR-2-IN-1 is a dual inhibitor of tubulin and VEGFR-2 (IC50 = 1.52 μM) with anti-angiogenic activity. Tubulin/VEGFR-2-IN-1 exhibits potent cytotoxicity against the cancer cells. Tubulin/VEGFR-2-IN-1 elevates ROS production, induces apoptosis and causes G0/G1 phase arrest in HepG-2 cells. Tubulin/VEGFR-2-IN-1 inhibits the migratory ability and the clonogenic ability in HepG-2 cells. Tubulin/VEGFR-2-IN-1 can be used for the study of cancer.
    Tubulin/VEGFR-2-IN-1
  • HY-W753201
    5'-Methylthioadenosine-13C
    5'-Methylthioadenosine-13C (5'-(Methylthio)-5'-deoxyadenosine-13C) is the 13C-labeled 5'-Methylthioadenosine (HY-16938). 5'-Methylthioadenosine (5'-(Methylthio)-5'-deoxyadenosine) is a nucleoside generated from S-adenosylmethionine (SAM) during polyamine synthesis. 5'-Methylthioadenosine suppresses tumors by inhibiting tumor cell proliferation, invasion, and the induction of apoptosis while controlling the inflammatory micro-environments of tumor tissue. 5'-Methylthioadenosine and its associated materials have striking regulatory effects on tumorigenesis.
    5'-Methylthioadenosine-<sup>13</sup>C
  • HY-186146A
    SGI-1776-VHL-02-epimer
    SGI-1776-VHL-02-epimer (SGI-1776-cis-VHL-02) is an epimer control compound of with SGI-1776-VHL-02 (HY-186146). SGI-1776-VHL-02-epimer has an inverted stereocenter in the critical hydroxyl-proline group in the VHL ligand. SGI-1776-VHL-02-epimer cannot trigger the VHL E3 ligase complex and does not degrade PIM1.
    SGI-1776-VHL-02-epimer
  • HY-N0667S7
    L-Asparagine-13C4,15N2
    L-Asparagine-13C4,15N2 ((-)-Asparagine-13C4,15N2) is the 13C and 15N-labeled L-Asparagine (HY-N0667). L-Asparagine is an essential amino acid for leukemic cells and a substrate for L-Asparaginase. L-Asparaginase is a potent anti-leukemic enzyme that promotes asparagine (Asn) and glutamine (Gln) depletion and inhibits protein biosynthesis in lymphoblasts. Removal of L-asparagine from plasma by L-Asparaginase results in inhibition of RNA and DNA synthesis and subsequent apoptosis. L-Asparaginase has cell-killing ability in vitro and in vivo, and selectively inhibits the growth of cancer cells with low asparagine synthetase (AASNS) expression. L-Asparagine can be used as a biomarker and sensor for the study of childhood acute lymphoblastic leukemia.
    L-Asparagine-<sup>13</sup>C<sub>4</sub>,<sup>15</sup>N<sub>2</sub>
  • HY-13065R
    Isobavachalcone (Standard)
    Inducer
    Isobavachalcone (Standard) is the analytical standard of Isobavachalcone. This product is intended for research and analytical applications. Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
    Isobavachalcone (Standard)
  • HY-B0116S
    Stavudine-d4
    Inducer
    Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
    Stavudine-d<sub>4</sub>
  • HY-18629A
    (E/Z)-SU9516
    Inducer
    (E/Z)-SU9516 is the isomer of SU9516 (HY-18629). SU9516 is a potent CDK2 inhibitor,with an IC50 of 22 nM,and also shows inhibitory effects on CDK1 and CDK4,with IC50s of 40,200 nM,respectively.
    (E/Z)-SU9516
  • HY-13468A
    KW-2478 hydrochloride
    Inducer
    KW-2478 hydrochloride is an HSP90 inhibitor (IC50 = 3.8 nM). KW-2478 hydrochloride inhibits the growth and induces apoptosis in chronic myeloid leukemia (CML) cells and liver cancer cells. KW-2478 hydrochloride weakens the BCR/ABL and MAPK signaling pathways, leading to increased p27 and p21 expression and decreased cyclin B1 expression. KW-2478 hydrochloride downregulates STAT3 expression. KW-2478 hydrochloride may be used in research on cancers such as CML and liver cancer.
    KW-2478 hydrochloride
  • HY-14584
    PQ-1
    Inducer
    PQ-1 is a gap junction enhancer.
    PQ-1
Cat. No. Product Name / Synonyms Application Reactivity