Cell apoptosis, sometimes called programmed cell death, is a cellular self-destruction method to remove old and damaged cells during development and aging to protect cells from external disturbances and maintain homeostasis. Apoptosis also occurs as a defense mechanism such as in immune reactions or when cells are damaged by disease or noxious agents.

Apoptosis is controlled by many genes and involves two fundamental pathways: the extrinsic pathway, which transmits death signals by the death receptor (DR), and the intrinsic or mitochondrial pathway. The extrinsic apoptotic pathway is activated by the binding of the death ligand to DRs, including FasL, TNF-α, and TRAIL, on the plasma membrane. The DR, adaptor protein (FADD), and associated apoptosis signaling molecule (caspase-8) form the death-inducing signaling complex (DISC), thus leading to the activation of the effector caspase cascade (caspase-3, -6, and -7). The mitochondria-mediated intrinsic apoptosis pathway is regulated by Bcl-2 family proteins, including proapoptotic (Bid, Bax, Bak) and antiapoptotic proteins (Bcl-2, Bcl-xL).

Abnormalities in cell apoptosis can be a significant component of diseases such as cancer, autoimmune lymphoproliferative syndrome, AIDS, ischemia, and neurode-generative diseases. These diseases may benefit from artificially inhibiting or activating apoptosis. A short list of potential methods of anti-apoptotic therapy includes stimulation of the IAP (inhibitors of apoptosis proteins) family of proteins, caspase inhibition, PARP (poly [ADP-ribose] polymerase) inhibition, stimulation of the PKB/Akt (protein kinase B) pathway, and inhibition of Bcl-2 proteins.

Ferroptosis and necroptosis are recently recognized forms of regulated cell death that differs considerably from apoptosis. Misregulated ferroptosis or necroptosis have also been implicated in multiple physiological and pathological processes, including cancer cell death, neurotoxicity, neurodegenerative diseases, etc.

References:
[1] Susan Elmore. Toxicol Pathol. 2007; 35(4): 495–516.
[2] Cao L, et al. J Cell Death. 2016 Dec 29;9:19-29.
[3] Dasgupta A, et al. Int J Mol Sci. 2017 Jan; 18(1): 23.
[4] Xie Y, et al. Cell Death Differ. 2016 Mar;23(3):369-79.


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FMK13918

CVT-11127 is a potent SCD inhibitor. CVT-11127 induces apoposis and arrests the cell cycle at the G1/S phase. CVT-11127 has the potential for the research of lung cancer[1].

  • CAS Number: 1018674-83-3
  • MF: C25H23Cl2N5O3
  • MW: 512.38800
  • Catalog: Apoptosis
  • Density: 1.39±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tigapotide

Tigapotide (PCK-3145) is an anti-tumour peptide that reduces the development of skeletal metastases associated with prostate cancer. Tigapotide induces apoptosis and reduces tumour parathyroid hormone-related peptide (PTHrP) levels[1].

  • CAS Number: 848084-83-3
  • MF: C82H119N21O34S3
  • MW: 2039.14000
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

a2e

Pyridinium bisretinoid A2E (A2E)is an initiator of blue-light-induced apoptosis. Photoactivation of Pyridinium bisretinoid A2E mediates autophagy and the production of reactive oxygen species[1][2].

  • CAS Number: 173449-96-2
  • MF: C42H58NO+
  • MW: 592.91600
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

diosbulbin d

Diosbulbin D is a potential hepatotoxic compound that can be isolated from Dioscorea bulbifera L.. Diosbulbin D induces apoptosis in L-02 cells[1].

  • CAS Number: 66756-57-8
  • MF: C19H20O6
  • MW: 344.36
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 599.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 316.2±30.1 °C

Mca-Asp-Glu-Val-Asp-Ala-Pro-Lys(Dnp)-OH

Mca-DEVDAP-K(Dnp)-OH is a fluorogenic substrate for caspase-3[1].

  • CAS Number: 189696-20-6
  • MF: C50H62N10O22
  • MW: 1155.08000
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ganoderenic acid D

Ganoderenic acid D is a triterpene identified from the effective compounds of Ganoderma lucidum extract (GLE). Ganoderenic acid D inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis[1].

  • CAS Number: 100665-43-8
  • MF: C30H40O7
  • MW: 512.634
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 702.3±60.0 °C at 760 mmHg
  • Melting Point: 218-220℃
  • Flash Point: 392.5±29.4 °C

Shikonine

Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin has shown various biological activities, including inhibition of TNF-α, NF-κB, HIV-1.

  • CAS Number: 517-89-5
  • MF: C16H16O5
  • MW: 288.295
  • Catalog: TNF Receptor
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 567.4±50.0 °C at 760 mmHg
  • Melting Point: 147ºC
  • Flash Point: 311.0±26.6 °C

Malabaricone B

Malabaricone B, a naturally occurring plant phenolic, is an orally active α-glucosidase inhibitor with an IC50 of 63.7 µM. Malabaricone B has anticancer, antimicrobial, anti-oxidation and antidiabetic activities[1][2][3].

  • CAS Number: 63335-24-0
  • MF: C21H26O4
  • MW: 342.43
  • Catalog: Apoptosis
  • Density: 1.17g/cm3
  • Boiling Point: 536.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 292.3ºC

SHR0302

SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects[1][2].

  • CAS Number: 1445987-21-2
  • MF: C18H22N8O2S
  • MW: 414.48
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BRD4 Degrader-17

PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells[1].

  • CAS Number: 2585561-49-3
  • MF: C49H47N7O9
  • MW: 877.94
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetrahydroxyquinone hydrate

Tetrahydroxyquinone hydrate (Tetrahydroxy-1,4-benzoquinone hydrate), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone hydrate can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS)[1].

  • CAS Number: 1215458-51-7
  • MF: C6H6O7
  • MW: 190.11
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

9-Oxo-10,11-dehydroageraphorone

Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells[1].

  • CAS Number: 79491-71-7
  • MF: C15H20O2
  • MW: 232.32
  • Catalog: Apoptosis
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 373.9±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 140.3±24.9 °C

ALA-ALA-PHE-CHLOROMETHYLKETONE TFA

AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research[1].

  • CAS Number: 102129-66-8
  • MF: C16H22ClN3O3
  • MW: 339.81700
  • Catalog: Apoptosis
  • Density: 1.215g/cm3
  • Boiling Point: 508.9ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 261.6ºC

HDAC1/CDK7-IN-1

HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells[1].

  • CAS Number: 2987905-95-1
  • MF: C33H32ClN7O4
  • MW: 626.10
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Polyphyllin B

Formosanin C is a diosgenin saponin isolated from Paris formosana Hayata and an immunomodulator with antitumor activity. Formosanin C induces apoptosis[1][2].

  • CAS Number: 50773-42-7
  • MF: C51H82O20
  • MW: 1015.185
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LYG-202

LYG-202, a flavonoid, has potent anti-angiogenic and antitumor activity. LYG-202 inhibits VEGF-stimulated HUVEC migration and tube formation. LYG-202 induces cancer cell apoptosis[1][2].

  • CAS Number: 1175077-25-4
  • MF: C25H30N2O5
  • MW: 438.51600
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nivalenol

Nivalenol, classified as type B trichotecenes toxins produced by Fusarium graminearum, is a fungal metabolite present in agricultural product[1]. Nivalenol induces cell death through caspase-dependent mechanisms and via the intrinsic apoptotic pathway. Nivalenol affects the immune system, causes emesis, growth retardation, reproductive disorders and has a haematotoxic/myelotoxic effect[2].

  • CAS Number: 23282-20-4
  • MF: C15H20O7
  • MW: 312.315
  • Catalog: Apoptosis
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 585.1±50.0 °C at 760 mmHg
  • Melting Point: 222-223ºC
  • Flash Point: 221.9±23.6 °C

trijuganone C

Trijuganone C, a natural product extracted from Salvia miltiorrhiza, inhibits the proliferation of cancer cells through induction of apoptosis mediated by mitochondrial dysfunction and caspase activation[1].

  • CAS Number: 135247-94-8
  • MF: C20H20O5
  • MW: 340.37
  • Catalog: Caspase
  • Density: 1.31g/cm3
  • Boiling Point: 502.1ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 221.5ºC

VisilizuMab

Visilizumab (Anti-Human CD3E Recombinant Antibody) is a humanized low-Fc receptor binding anti-CD3 monoclonal IgG2 antibody. Visilizumab can be used for ulcerative colitis and Crohn's disease research[1].

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VS 8

VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells)[1].

  • CAS Number: 2471865-38-8
  • MF: C26H20F3N3O3
  • MW: 479.45
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-(3-Phenoxybenzyl)amino-β-carboline

3-(3-Phenoxybenzyl)amino-β-carboline is a potent tubulin inhibitor. 3-(3-Phenoxybenzyl)amino-β-carboline promotes selective degradation of αβ-tubulin heterodimers. 3-(3-Phenoxybenzyl)amino-β-carboline induces G2/M phase cell cycle arrest and apoptosis. 3-(3-Phenoxybenzyl)amino-β-carboline exhibits anticancer activity[1].

  • CAS Number: 1327080-54-5
  • MF: C24H19N3O
  • MW: 365.43
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

koenimbine

Koenimbine is an anticancer agent that can be obtained from the leaves and fruits of Murraya koenigii. Koenimbine can induce apoptosis and necrosis in HT-29 and SW48 cells. Koenimbine can be used in the research of cancer[1].

  • CAS Number: 21087-98-9
  • MF: C19H19NO2
  • MW: 293.36
  • Catalog: Apoptosis
  • Density: 1.193g/cm3
  • Boiling Point: 482.1ºC at 760 mmHg
  • Melting Point: 194-195℃
  • Flash Point: 171.8ºC

(-)-Irofulven

(-)-Irofulven (MGI 114), an Illudin S analog, is a DNA alkylating agent. (-)-Irofulven inhibits the replication of DNA, induces tumor cells apoptosis, and has potent antitumor activity[1][2].

  • CAS Number: 158440-71-2
  • MF: C15H18O3
  • MW: 246.30200
  • Catalog: Apoptosis
  • Density: 1.28g/cm3
  • Boiling Point: 501ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 270.9ºC

GNE-900

GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity[1].

  • CAS Number: 1200126-26-6
  • MF: C23H21N5
  • MW: 367.446
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 633.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 336.9±31.5 °C

m-3M3FBS

m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis[1][2][3].

  • CAS Number: 200933-14-8
  • MF: C16H16F3NO2S
  • MW: 343.36400
  • Catalog: Apoptosis
  • Density: 1.316g/cm3
  • Boiling Point: 420ºC at 760mmHg
  • Melting Point: 114-114.8ºC(lit.)
  • Flash Point: 207.8ºC

GSK'481

GSK'481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cellsGSK'481 have approximately equivalent RIP1 FP potencies against human andcynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP1

  • CAS Number: 1622849-58-4
  • MF: C21H19N3O4
  • MW: 377.393
  • Catalog: RIP kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 677.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 363.2±31.5 °C

20(R)-Ginsenoside Rh2

20(R)-Ginsenoside Rh2, a matrix metalloproteinase (MMP) inhibitor, acts as a cell antiproliferator. It has anticancer effects via blocking cell proliferation and causing G1 phase arrest. 20(R)-Ginsenoside Rh2 induces apoptosis, and has anti-inflammatory and antioxidative activity[1][2][3].

  • CAS Number: 112246-15-8
  • MF: C36H62O8
  • MW: 622.873
  • Catalog: Apoptosis
  • Density: 1.19
  • Boiling Point: 726.4±60.0 °C at 760 mmHg
  • Melting Point: 225 °C
  • Flash Point: 393.1±32.9 °C

Multi-kinase-IN-2

Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity[1].

  • CAS Number: 2095628-21-8
  • MF: C34H35N5O3
  • MW: 561.67
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pioglitazone (potassium salt)

Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research[2][3][4].

  • CAS Number: 1266523-09-4
  • MF: C19H19KN2O3S
  • MW: 394.529
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hypocretin (70-98) (human)

Hypocretin (70-98), human is a polypeptide that is capable of binding to an orexin receptor OX1R and promotes Apoptosis[1].

  • CAS Number: 1129545-33-0
  • MF: C125H214N44O37S
  • MW: 2957.374
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A