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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Mcl1-IN-2

Mcl1-IN-2 is an inhibitor of myeloid cell factor 1 (Mcl-1).

  • CAS Number: 292057-76-2
  • MF: C19H15N3OS
  • MW: 333.407
  • Catalog: Bcl-2 Family
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 557.5±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 290.9±28.7 °C

L-Ascorbic acid-13C-2

L-Ascorbic acid-13C-2 is the 13C labeled L-Ascorbic acid. L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen

  • CAS Number: 1313730-17-4
  • MF: C513CH8O6
  • MW: 177.12
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ciclopirox Olamine

Ciclopirox olamine is a synthetic antifungal agent for topical dermatologic treatment of superficial mycoses. It is most useful against Tinea versicolor.

  • CAS Number: 41621-49-2
  • MF: C14H24N2O3
  • MW: 268.352
  • Catalog: Bacterial
  • Density: N/A
  • Boiling Point: 350ºC at 760 mmHg
  • Melting Point: 144ºC
  • Flash Point: 165.5ºC

7-epi-Isogarcinol

7-epi-Isogarcinol is a polycyclic polyprenylated acylphloroglucinol (PPAP), with moderate antiproliferative activity. 7-epi-Isogarcinol blocks STAT3 signaling pathway, to induce apoptosis and inhibit cell migration[1].

  • CAS Number: 1141378-40-6
  • MF: C38H50O6
  • MW: 602.80
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Physalin B

Physalin B, one of the major active steroidal constituents of Cape gooseberry, induces cell cycle arrest and triggers apoptosis in breast cancer cells through modulating p53-dependent apoptotic pathway. Physalin B inhibits the ubiquitin-proteasome pathway and induces incomplete autophagic response in human colon cancer cells in vitro[1][2].

  • CAS Number: 23133-56-4
  • MF: C28H30O9
  • MW: 510.53200
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Jolkinolide B

Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells[1].

  • CAS Number: 37905-08-1
  • MF: C20H26O4
  • MW: 330.418
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 497.1±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 219.8±28.8 °C

caspase-8 inhibitor

Ac-?IETD-?CHO is a potent, reversible inhibitor of granzyme B and caspase-8. Ac-?IETD-?CHO inhibits Fas-mediated apoptotic cell death, hemorrhage, and liver failure. Ac-?IETD-?CHO also inhibits cytotoxic T lymphocytes induced cell death[1][2].

  • CAS Number: 191338-86-0
  • MF: C21H34N4O10
  • MW: 502.516
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 971.9±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 541.6±34.3 °C

RIP1 kinase inhibitor 8

RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC50 of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species[1].

  • CAS Number: 2226735-54-0
  • MF: C18H19F2N5O2
  • MW: 375.37
  • Catalog: RIP kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HDAC1/2 and CDK2-IN-1

HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity[1].

  • CAS Number: 2418559-01-8
  • MF: C26H22ClN7O
  • MW: 483.95
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ro 24-7429

Ro24-7429 is a potent and orally active HIV-1 transactivator protein Tat antagonist. Ro24-7429 is also a runt-related transcription factor 1 (RUNX1) inhibitor. Ro24-7429 has anti-HIV, antifibrotic and anti-inflammatory effects[1][2].

  • CAS Number: 139339-45-0
  • MF: C14H13ClN4
  • MW: 272.73300
  • Catalog: HIV
  • Density: 1.36g/cm3
  • Boiling Point: 514.6°C(760mmHg),计算值
  • Melting Point: N/A
  • Flash Point: 265°C

Hexapeptide-11

Hexapeptide-11 is a bioactive peptide with anti-aging effect. Hexapeptide-11 protects fibroblasts against oxidative stress-mediated premature cellular senescence by mediating a downregulation of cellular proteins, such as ataxia telangiectasia mutated (ATM) and p53 [1].

  • CAS Number: 161258-30-6
  • MF: C36H48N6O7
  • MW: 676.80200
  • Catalog: MDM-2/p53
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YVAD-CHO

YVAD-CHO is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor that can partially delay motoneurone death in lesioned facial nerve mice[1].

  • CAS Number: 153604-27-4
  • MF: C21H30N4O7
  • MW: 450.49
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Minnelide

Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide causes apoptotic[1].

  • CAS Number: 1254702-87-8
  • MF: C21H25Na2O10P
  • MW: 514.37
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Licofelone-d6

Licofelone-d6 is the deuterium labeled Licofelone[1]. Licofelone (ML-3000) is a dual COX/5-lipoxygenase (5-LOX) inhibitor (IC50=0.21/0.18 μM, respectively) for the treatment of osteoarthritis. Licofelone exerts anti-inflammatory and anti-proliferative effects. Licofelone induces apoptosis, and decreases the production of proinflammatory leukotrienes and prostaglandins[2][3][4].

  • CAS Number: 1178549-81-9
  • MF: C23H16D6ClNO2
  • MW: 385.92
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

c-Met-IN-14

c-Met-IN-14 (compound 26af) is a selective inhibitor of c-Met kinase from N-sulfonylamidine-based derivatives, with an IC50 value of 2.89 nM. c-Met-IN-14 shows anticancer activity by blocking phosphorylation of c-Met, and arrests cell cycle at G2/M phase. c-Met-IN-14 induces apoptosis of A549 cells in a dose-dependent manner[1].

  • CAS Number: 2443380-34-3
  • MF: C34H38ClFN4O7S
  • MW: 701.20
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

isodispar B

Isodispar B is an anticancer agent that inhibits the proliferation of nasopharyngeal carcinoma and breast cancer cells and induces cell apoptosis. Isodispar B is cytotoxic to a wide range of cancer cell lines[1].

  • CAS Number: 98192-64-4
  • MF: C20H18O5
  • MW: 338.35400
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

RIPK2-IN-8

RIPK-IN-4 is a potent and selective RIPK2 inhibitor with excellent oral bioavailability, and has an IC50 of 3 nM[1].

  • CAS Number: 2141969-56-2
  • MF: C18H21FN4O3S
  • MW: 392.45
  • Catalog: RIP kinase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiocolchicine-d3

Thiocolchicine-d3 is deuterium labeled Thiocolchicine. Thiocolchicine, a derivative modified in the C Ring of Colchicine (HY-16569) with enhanced biological properties. Thiocolchicine is a potent inhibitor of tubulin polymerization (IC50=2.5 µM) and competitively binds to tubulin with a Ki of 0.7 µM. Thiocolchicine induces cell apoptosis[1][2]. Thiocolchicine can be used as an ADC cytotoxin in ADC technology.

  • CAS Number: 1314417-95-2
  • MF: C22H22D3NO5S
  • MW: 418.52
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cu(II)-Elesclomol

Cu(II)-Elesclomol is a Cu2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces apoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity[1].

  • CAS Number: 1224195-72-5
  • MF: C19H18CuN4O2S2
  • MW: 462.05
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TS-IN-2

TS-IN-2 (compound 17) is a thymidylate synthase (TS) inhibitor with an IC50 of 0.81 μM. TS-IN-2 induces cancer cell apoptosis and cell cycle arrest in S phase, and also inhibit DNA synthesis, resulting in DNA damage[1].

  • CAS Number: 2945983-00-4
  • MF: C18H23N3O4S
  • MW: 377.46
  • Catalog: Thymidylate Synthase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Oxaprozin, potassium salt

Oxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties[1][2].

  • CAS Number: 174064-08-5
  • MF: C18H14KNO3
  • MW: 331.40700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: 467ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 236.2ºC

Necrostatin-7

Necrotatin-7 (Nec-7) is a potent necroptosis inhibitor with an EC50 of 10.6 μM. Necrotatin-7 does not inhibit recombinant RIP1 kinase[1].

  • CAS Number: 351062-08-3
  • MF: C16H10FN5OS2
  • MW: 371.412
  • Catalog: Apoptosis
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: 613.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 324.8±34.3 °C

PD 166285 dihydrochloride

PD0166285 dihydrochloride, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50 of 3.433 μM for Chk1[1].

  • CAS Number: 212391-63-4
  • MF: C26H28Cl3N5O2
  • MW: 548.89200
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: 239-242?C
  • Flash Point: N/A

Mafosfamide Sodium Salt

Mafosfamide sodium salt (Z 7557 sodium salt) targets nuclear DNA, forms DNA cross-links and inhibits DNA synthesis. Mafosfamide sodium salt, a cyclophosphamide analogue, induces apoptosis in lymphoblastoid cells. Mafosfamide sodium salt has antitumor activity[1][2].

  • CAS Number: 84211-05-2
  • MF: C9H18Cl2N2NaO5PS2
  • MW: 401.26700
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Paeoniflorigenone

Paeoniflorigenone, isolated as an active ingredient from the root of moutan cortex, induces apoptosis selectively in the cancer cell lines and exhibits antiproliferative effect[1].

  • CAS Number: 80454-42-8
  • MF: C17H18O6
  • MW: 318.321
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 481.1±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 177.1±22.2 °C

Ac-Val-Asp-Val-Ala-Asp-pNA

Ac-VDVAD-pNA is a caspase-2 substrate. Ac-VDVAD-pNA can be used to test the activity of caspase-2[1].

  • CAS Number: 189684-53-5
  • MF: C29H41N7O12
  • MW: 679.675
  • Catalog: Caspase
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 1160.8±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 655.8±34.3 °C

BCH

LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis[1][2][3].

  • CAS Number: 20448-79-7
  • MF: C8H13NO2
  • MW: 155.19400
  • Catalog: Apoptosis
  • Density: 1.256g/cm3
  • Boiling Point: 295.5ºC at 760 mmHg
  • Melting Point: >300 °C(lit.)
  • Flash Point: 132.5ºC

VEGFR-2-IN-19

VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent[1].

  • CAS Number: 2456315-41-4
  • MF: C21H19N3O2
  • MW: 345.39
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Zoledronic Acid, Disodium Salt, Tetrahydrate

Zoledronic Acid (Zoledronate) disodium tetrahydrate is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid disodium tetrahydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid disodium tetrahydrate also has anti-cancer effects[1].

  • CAS Number: 165800-07-7
  • MF: C5H16N2Na2O11P2
  • MW: 388.11400
  • Catalog: Apoptosis
  • Density: 2.13g/cm3
  • Boiling Point: 764ºC at 760mmHg
  • Melting Point: 305-307ºC
  • Flash Point: 415.8ºC

Diallyl trisulfide

Diallyl Trisulfide is isolated from Garlic. Diallyl Trisulfide suppresses the growth of Penicillium expansum (MFC99 value: ≤ 90 μg/mL) and promotes apoptosis via production of reactive oxygen species (ROS) and disintegration of cellular ultrastructure. Anticancer effect[1].

  • CAS Number: 2050-87-5
  • MF: C6H10S3
  • MW: 178.339
  • Catalog: Fungal
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 229.5±43.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 87.8±25.2 °C