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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15-PGDH 5 alpha Reductase 5-Lipoxygenase Acetyl-CoA Carboxylase Acyltransferase Adenosine Deaminase Adenosine Kinase Aldehyde Dehydrogenase (ALDH) Aldose Reductase Aminopeptidase Angiotensin-converting Enzyme (ACE) ATGL ATP Citrate Lyase Carbonic Anhydrase Carboxypeptidase Cathepsin CETP COMT Cytochrome P450 Dipeptidyl Peptidase Dopamine β-hydroxylase E1/E2/E3 Enzyme Elastase Enolase FAAH FABP Factor Xa Farnesyl Transferase Fatty Acid Synthase (FAS) FXR Glucokinase GSNOR Gutathione S-transferase HCV Protease Hexokinase HIF/HIF Prolyl-Hydroxylase HIV Integrase HIV Protease HMG-CoA Reductase (HMGCR) HSP Indoleamine 2,3-Dioxygenase (IDO) Isocitrate Dehydrogenase (IDH) Lactate Dehydrogenase LXR MAGL Mineralocorticoid Receptor Mitochondrial Metabolism MMP Nampt NEDD8-activating Enzyme Neprilysin PAI-1 PDHK PGC-1α Phosphatase Phosphodiesterase (PDE) Phospholipase Procollagen C Proteinase Proteasome Pyruvate Kinase RAR/RXR Renin ROR Ser/Thr Protease SGK Stearoyl-CoA Desaturase (SCD) Thrombin Tryptophan Hydroxylase Tyrosinase Xanthine Oxidase
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Abacavir (sulfate)

Abacavir monosulfate is a competitive, orally active nucleoside reverse transcriptase inhibitor. Abacavir monosulfate can inhibits the replication of HIV. Abacavir monosulfate shows anticancer activity in prostate cancer cell lines. Abacavir monosulfate can trespass the blood-brain-barrier and suppresses telomerase activity[1][2][3].

  • CAS Number: 216699-07-9
  • MF: C14H20N6O5S
  • MW: 384.411
  • Catalog: HIV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hsp90-Cdc37-IN-3

Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis[1].

  • CAS Number: 2361009-68-7
  • MF: C35H44ClN3O6
  • MW: 638.19
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PDK4-IN-1

PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].

  • CAS Number: 2310262-10-1
  • MF: C22H19N3O2
  • MW: 357.41
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Shikonin

Alkannin, found in Alkanna tinctoria, is used as a food coloring. Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. Alkannin improves hepatic inflammation in a Rho-kinase pathway[1][2][3].

  • CAS Number: 517-88-4
  • MF: C16H16O5
  • MW: 288.295
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 567.4±50.0 °C at 760 mmHg
  • Melting Point: 149°
  • Flash Point: 311.0±26.6 °C

pan-HER-IN-2

pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFRT790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities[1].

  • CAS Number: 1639040-95-1
  • MF: C19H15BrClN5O
  • MW: 444.71
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tamoxifen-d5

Tamoxifen-d5 (ICI 47699-d5) is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is a selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity[1][2].

  • CAS Number: 157698-32-3
  • MF: C26H24D5NO
  • MW: 376.54500
  • Catalog: Apoptosis
  • Density: 1.057g/cm3
  • Boiling Point: 482.3ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 140ºC

Mcl1-IN-4

Mcl1-IN-4 is an inhibitor of Mcl1 with an IC50 of 0.2 μM.

  • CAS Number: 1580484-04-3
  • MF: C28H26N2O5S
  • MW: 502.58
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Z-VAD(OMe)-FMK

Z-VAD(OMe)-FMK is a cell-permeable and irreversible pan-caspase inhibitor.

  • CAS Number: 187389-52-2
  • MF: C22H30FN3O7
  • MW: 467.488
  • Catalog: Peptides
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 732.4±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 396.7±32.9 °C

ZYZ-488

ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor, which inhibits the activation of binding protein procaspase-9 and procaspase-3[1].

  • CAS Number: 1470302-79-4
  • MF: C20H29N3O11
  • MW: 487.46
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RMS3

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[1].

  • CAS Number: 2497686-66-3
  • MF: C38H39F3N2O6
  • MW: 676.72
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Anticancer agent 55

Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer[1].

  • CAS Number: 2408800-91-7
  • MF: C28H21Br2FN2O2
  • MW: 596.28
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ZIO 101

Darinaparsin (ZIO-101), an organic arsenical, is a mitochondrial-targeted agent. Darinaparsin induces apoptosis in ancer cells, and has anticancer effects[1].

  • CAS Number: 69819-86-9
  • MF: C12H22AsN3O6S
  • MW: 411.30600
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PI3K/AKT-IN-2

PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin[1].

  • CAS Number: 2684412-41-5
  • MF: C32H27BrO10
  • MW: 651.45
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bendamustine-d8 hydrochloride

Bendamustine-d8 (hydrochloride) is deuterium labeled Bendamustine (hydrochloride). Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties[1].

  • CAS Number: 1185068-23-8
  • MF: C16H14D8Cl3N3O2
  • MW: 402.77
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sodium 4-Phenylbutyrate-d11

Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].

  • CAS Number: 1392208-11-5
  • MF: C10D11NaO2
  • MW: 197.25
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thailanstatin D

Thailanstatin D, an analogue of Thailanstatin A, is able to inhibit AR-V7 gene splicing by interfering the interaction between U2AF65 and SAP155 and preventing them from binding to polypyrimidine tract located between the branch point and the 3' splice site. Thailanstatin D exhibits a potent tumor inhibitory effect on human CRPC xenografts leading to cell apoptosis[1].

  • CAS Number: 1609105-89-6
  • MF: C28H41NO8
  • MW: 519.63
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mcl-1 inhibitor 8

Mcl-1 inhibitor 8 is a MCL-1 inhibitor, example 228, extracted from patent WO2019222112[1].

  • CAS Number: 2388471-31-4
  • MF: C38H46ClN5O6S
  • MW: 736.32
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC HDAC6 degrader 1

PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines[1].

  • CAS Number: 2785404-76-2
  • MF: C37H46N6O10
  • MW: 734.80
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-Aminolevulinic acid-4-13C hydrochloride

5-Aminolevulinic acid-4-13C (hydrochloride) is the 13C labeled 5-Aminolevulinic acid hydrochloride[1]. 5-Aminolevulinic acid hydrochloride (5-ALA hydrochloride) is an intermediate in heme biosynthesis in the body and the universal precursor of tetrapyrroles[2][3].

  • CAS Number: 129720-94-1
  • MF: C413CH10ClNO3
  • MW: 168.58
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AX-024

AX-024 is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.

  • CAS Number: 1370544-73-2
  • MF: C21H22FNO2
  • MW: 339.40
  • Catalog: TNF Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pifithrin-β (hydrobromide)

Pifithrin-β is a potent p53 inhibitor with an IC50 of 23 μM.

  • CAS Number: 511296-88-1
  • MF: C16H17BrN2S
  • MW: 349.289
  • Catalog: MDM-2/p53
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sinomenine

Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation[1]. Sinomenine also is an activator of μ-opioid receptor[2].

  • CAS Number: 115-53-7
  • MF: C19H23NO4
  • MW: 329.390
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 513.6±50.0 °C at 760 mmHg
  • Melting Point: 180ºC
  • Flash Point: 264.4±30.1 °C

9-cis-Retinoic acid-d5

9-cis-Retinoic acid-d5 (ALRT1057-d5) is the deuterium labeled 9-cis-Retinoic acid. 9-cis-Retinoic acid (ALRT1057), a vitamin A derivative, is a potent RAR/RXR agonist. 9-cis-Retinoic acid induces apoptosis, regulates cell cycle and has anticancer, anti-inflammatory and neuroprotection activities[1][2][3][4][5][6].

  • CAS Number: 78996-15-3
  • MF: C20H23D5O2
  • MW: 305.47
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fascaplysin (chloride)|CDK4 inhibitor

Fascaplysin is an antimicrobial and cytotoxic red pigment, that can come from the marine sponge (Fascaplysinopsis sp.). Fascaplysin has been synthesized in seven steps from indole (65% yield). Fascaplysin can induces apoptosis and autophagy in human leukemia HL-60 cells. Fascaplysin shows anti-tumor activity[1][2].

  • CAS Number: 114719-57-2
  • MF: C18H11ClN2O
  • MW: 306.75
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

ICCB280

ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc)[1][2].

  • CAS Number: 2041072-41-5
  • MF: C23H18N2O4
  • MW: 386.400
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 624.1±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 331.2±34.3 °C

aspidin BB

Aspidin BB is a phloroglucinol derivative, which can be isolated from the aerial part of Dryopteris championii. Aspidin BB has anticancer activity. Aspidin BB induces cell cycle arrest and apoptosis in human ovarian HO-8910 cells[1][2].

  • CAS Number: 584-28-1
  • MF: C25H32O8
  • MW: 460.51700
  • Catalog: Apoptosis
  • Density: 1.285g/cm3
  • Boiling Point: 704.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 236.6ºC

gn25

GN25 is a specific p53-Snail binding inhibitor with antitumor effects[1].

  • CAS Number: 1227401-27-5
  • MF: C15H14O6S
  • MW: 322.333
  • Catalog: MDM-2/p53
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 608.4±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 321.7±31.5 °C

GSK 583

GSK583 is a highly potent and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM.

  • CAS Number: 1346547-00-9
  • MF: C20H19FN4O2S
  • MW: 398.454
  • Catalog: RIP kinase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 652.9±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 348.7±31.5 °C

Ropeginterferon alfa-2b

Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft) is a monopegylated IFN-α that can be used for the research of myeloproliferative neoplasms[1].

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

HDAC-IN-60

HDAC-IN-60 (compound 21a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-60 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis[1].

  • CAS Number: 2944459-58-7
  • MF: C20H26N2O6
  • MW: 390.43
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A