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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Etanercept

Etanercept (Enbrel) is a tumor necrosis factor (TNF) inhibitor used for treating rheumatoid arthritis, ankylosing spondylitis, psoriatic arthritis and plaque psoriasis.

  • CAS Number: 185243-69-0
  • MF: C2224H3475N621O698S36
  • MW: 116.97816
  • Catalog: TNF Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Calcimycin hemicalcium salt

Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation of mammalian cells. Calcimycin hemicalcium salt induces apoptosis[1][2][3][4].

  • CAS Number: 59450-89-4
  • MF: C58H72CaN6O12
  • MW: 1085.303
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Balanophonin

Balanophonin is an anti-inflammatory and anti-cancer agent. Balanophonin inhibits microglial activation and neurodegeneration via inhibiting activated microglia-induced apoptosis[1].

  • CAS Number: 80286-36-8
  • MF: C20H20O6
  • MW: 356.36900
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AEG 3482

AEG3482 is a potent antiapoptotic compound that inhibits Jun kinase (JNK) activity through induced expression of heat shock protein 70 (HSP70). AEG3482 directly binds HSP90, thereby facilitating HSF1-dependent expression of HSP70 and HSP25[1].

  • CAS Number: 63735-71-7
  • MF: C10H8N4O2S2
  • MW: 280.326
  • Catalog: Apoptosis
  • Density: 1.8±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lepadin H

Lepadin H is a marine alkaloid and ferroptosis inducer. Lepadin H exhibits significant cytotoxicity, promotes p53 expression, increases ROS production and lipid peroxidation, decreases SLC7A11 and GPX4 levels, and upregulates ACSL4 expression. Lepadin H induces ferroptosis through the p53-SLC7A11-GPX4 pathway[1].

  • CAS Number: 412328-25-7
  • MF: C26H45NO3
  • MW: 419.64
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

KYP 2047

KYP-2047 is a potent and BBB-penetrating prolyl-oligopeptidase (POP) inhibitor, with an Ki value of 0.023 nM. KYP-2047 reduces glioblastoma proliferation through angiogenesis and apoptosis modulation[1][2].

  • CAS Number: 796874-99-2
  • MF: C20H25N3O2
  • MW: 339.43
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PK68

PK68 is a potent and selective type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis. PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and with great potential for use in the treatment of inflammatory disorders and cancer metastasis[1].

  • CAS Number: 2173556-69-7
  • MF: C22H24N4O3S
  • MW: 424.52
  • Catalog: RIP kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LY 303511

LY303511 is a structural analogue of LY294002. LY303511 does not inhibit PI3K. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells. LY303511 reversibly blocks K+ currents (IC50=64.6±9.1 μM) in MIN6 insulinoma cells.

  • CAS Number: 154447-38-8
  • MF: C19H18N2O2
  • MW: 306.358
  • Catalog: TNF Receptor
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 496.1±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 253.8±28.7 °C

Butylated hydroxytoluene-d21

Butylated hydroxytoluene-d21 is the deuterium labeled Butylated hydroxytoluene[1]. Butylated hydroxytoluene is an antioxidant widely used in foods and in food-related products[2]. Butylated hydroxytoluene is a Ferroptosis inhibitor[3].

  • CAS Number: 64502-99-4
  • MF: C15H3D21O
  • MW: 241.48000
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: 265ºC(lit.)
  • Melting Point: 69-71ºC(lit.)
  • Flash Point: N/A

7,8,9,9-Tetradehydroisolariciresinol

Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively[1].

  • CAS Number: 357645-16-0
  • MF: C20H20O6
  • MW: 356.369
  • Catalog: Bcl-2 Family
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 587.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 211.0±23.6 °C

SW106065

SW106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST). SW106065 inhibits ATP consumption of sMPNST and other models of MPNST with an EC50 of 1 µM. SW106065 can be used for MPNST research[1].

  • CAS Number: 62289-81-0
  • MF: C10H8N2OS
  • MW: 204.24800
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BI-0252

BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis[1].

  • CAS Number: 1818291-27-8
  • MF: C30H26Cl2FN3O3
  • MW: 566.45
  • Catalog: MDM-2/p53
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Deracoxib-d3

Deracoxib-d3 is the deuterium labeled Deracoxib. Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID).

  • CAS Number: 2012598-48-8
  • MF: C17H11D3F3N3O3S
  • MW: 400.39
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCH 79797 dihydrochloride

SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].

  • CAS Number: 1216720-69-2
  • MF: C23H27Cl2N5
  • MW: 444.400
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VTP50469 fumarate

VTP50469 fumarate is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 fumarate has potently anti-leukemia activity[1][2].

  • CAS Number: 2169919-29-1
  • MF: C32H47FN6O4S.3/2C4H4O4
  • MW: 804.93
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-(2,4-Dichlorophenyl)-1,4-dihydro-[1,3,5]triazino[1,2-a]benzimidazol-2-amine

Topoisomerase II inhibitor 14 (compound 2f) is a potent inhibtor of Topoisomerase II, with anticancer activity. Topoisomerase II inhibitor 14 induces apoptosis, and arrests cell cycle at S phase. Topoisomerase II inhibitor 14 exhibits antioxidant effect and decreases the level of GSH, MDA, and NO[1].

  • CAS Number: 305343-00-4
  • MF: C15H11Cl2N5
  • MW: 332.19
  • Catalog: Apoptosis
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 493.6±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 252.3±31.5 °C

Taurochenodeoxycholic acid

Taurochenodeoxycholic acid is one of the main bioactive substances of animals' bile acid.

  • CAS Number: 516-35-8
  • MF: C26H45NO6S
  • MW: 499.704
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pseudolaric acid B

Pseudolaric Acid B is a diterpene isolated from the root of Pseudolarix kaempferi Gorden (pinaceae), has anti-cancer, antifungal, and antifertile activities, and shows immunosuppressive activity on T lymphocytes[1][2][3]. Pseudolaric Acid B inhibits hepatitis B virus (HBV) secretion through apoptosis and cell cycle arrest. Pseudolaric Acid B induces autophagy[4][5].

  • CAS Number: 82508-31-4
  • MF: C23H28O8
  • MW: 432.464
  • Catalog: Fungal
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 613.8±55.0 °C at 760 mmHg
  • Melting Point: 166°C
  • Flash Point: 208.8±25.0 °C

L-Glutamine-15N-1

L-Glutamine-15N-1 (L-Glutamic acid 5-amide-15N-1) is the 15N-labeled L-Glutamine. L-Glutamine (L-Glutamic acid 5-amide) is a non-essential amino acid present abundantly throughout the body and involved in many metabolic processes. L-Glutamine provides a source of carbons for oxidation in some cells[1][2].

  • CAS Number: 59681-32-2
  • MF: C5H10N15NO3
  • MW: 146.145
  • Catalog: Ferroptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 445.6±40.0 °C at 760 mmHg
  • Melting Point: 185ºC (dec.)(lit.)
  • Flash Point: 223.3±27.3 °C

GPR

GPR is a three amino acid peptide. GPR can rescue cultured rat hippocampal neurons from Aβ-induced neuronal death by inhibiting caspase-3/p53 dependent apoptosis. GPR can be used for the research of Alzheimer's disease (AD).

  • CAS Number: 47295-77-2
  • MF: C13H24N6O4
  • MW: 328.36700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DNMT3A-IN-2

DNMT3A-IN-2 (compound 2) is a potent and allosteric inhibitor of DNMT3A. DNMT3A-IN-2 inhibits DNMT3A activity by disrupting protein-protein interactions. DNMT3A-IN-2 induces apoptosis of acute myeloid leukemia (AML) cell lines. DNMT3A-IN-2 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882[1].

  • CAS Number: 2366272-43-5
  • MF: C33H40N6O4
  • MW: 584.71
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RIP2 kinase inhibitor 1

RIP2 kinase inhibitor 1 is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

  • CAS Number: 1423186-80-4
  • MF: C21H22N4O4S2
  • MW: 458.554
  • Catalog: RIP kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 719.9±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 389.2±32.9 °C

ζ-Stat

ζ-Stat (NSC37044) is a specific and atypical PKC-ζ inhibitor, with an IC50 of 5 μM. ζ-Stat can reduce melanoma cell lines proliferation and induce apoptosis, and has antitumor activity in vitro[1][2].

  • CAS Number: 3316-02-7
  • MF: C10H8O10S3
  • MW: 384.36000
  • Catalog: Apoptosis
  • Density: 2.019g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Concanavalin A

Concanavalin A is a Ca2+/Mn2+-dependent and mannose/glucose-binding plant lectin that can be found in jack bean. Concanavalin A can induce programmed cell death[1].

  • CAS Number: 11028-71-0
  • MF: C15H24
  • MW: 304.35
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 39 °C

Nampt-IN-3

Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death[1].

  • CAS Number: 2121591-52-2
  • MF: C29H25N7O2
  • MW: 503.55
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(R)-2-AMINO-3-(PROP-2-YN-1-YLTHIO)PROPANOIC ACID

S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties[1][2].

  • CAS Number: 3262-64-4
  • MF: C6H9NO2S
  • MW: 159.21
  • Catalog: MDM-2/p53
  • Density: 1.284g/cm3
  • Boiling Point: 294.8ºC at 760 mmHg
  • Melting Point: 176-178 °C
  • Flash Point: 132.1ºC

1',4"-Sophorolactone 6',6"-diacetate

Lactonic sophorolipid is a natural antimicrobial surfactant for oral hygiene[1]. Lactonic sophorolipid, a potential anticancer agent, induces apoptosis in human HepG2 cells through the caspase-3 pathway[1].

  • CAS Number: 148409-20-5
  • MF: C34H56O14
  • MW: 688.800
  • Catalog: Bacterial
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 843.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 256.9±27.8 °C

L-Cystine-34S2

L-Cystine-34S2 is the 34S-labeled L-Cystine. L-Cystine is an amino acid and intracellular thiol, which plays a critical role in the regulation of cellular processes.

  • CAS Number: 113512-08-6
  • MF: C6H12N2O434S2
  • MW: 244.11
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TC ASK 10

TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].

  • CAS Number: 1005775-56-3
  • MF: C21H23Cl2N5O
  • MW: 432.346
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Coenzyme Q10-d6

Coenzyme Q10-d6 is deuterium labeled Coenzyme Q10. Coenzyme Q10 is an essential cofactor of the electron transport chain and a potent antioxidant agent.

  • CAS Number: 110971-02-3
  • MF: C59H84D6O4
  • MW: 869.38
  • Catalog: Ferroptosis
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 869.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 324.6±34.3 °C