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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Anticancer agent 99

Anticancer agent 99 (compound 2p) has good anticancer activity against HepG2 cells, with an IC50 value of 35.9 μM. Anticancer agent 99 can induce apoptosis and has anti-proliferation effect[1].

  • CAS Number: 2914922-83-9
  • MF: C19H20F3N3O2
  • MW: 379.38
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydrolyzed Fumonisin B1

Hydrolyzed Fumonisin B1 (Aminopentol) is the backbone and main hydrolysis product of the mycotoxin fumonisin B1 (FB1), can weakly inhibit ceramide synthase[1].

  • CAS Number: 145040-09-1
  • MF: C22H47NO5
  • MW: 405.61200
  • Catalog: Apoptosis
  • Density: 1.051±0.06 g/cm3(Predicted)
  • Boiling Point: 593.8±50.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: N/A

Pyoluteorin

Pyoluteorin is an antibiotic that inhibits Oomycete fungi, including the plant pathogen Pythium ultimum, and suppresses plant diseases caused by this fungus[1]. Pyoluteorin induces human triple-negative breast cancer MDA-MB-231 cells apoptosis in vitro. Pyoluteorin can be used for the research of human triple-negative breast cancer[2].

  • CAS Number: 25683-07-2
  • MF: C11H7Cl2NO3
  • MW: 272.08400
  • Catalog: Fungal
  • Density: 1.632g/cm3
  • Boiling Point: 436.9ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 218ºC

Butylated hydroxytoluene-d3

Butylated hydroxytoluene-d3 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: 86819-59-2
  • MF: C15H21D3O
  • MW: 223.37
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tolbutamide Sodium

Tolbutamide sodium is a potent and orally active antidiabetic agent. Tolbutamide sodium induces apoptosis in a Ca2+ dependent manner in pancreatic β-cells. Tolbutamide sodium has the potential for the research of non-insulin-dependent diabetes mellitus[1][2].

  • CAS Number: 473-41-6
  • MF: C12H18N2O3S
  • MW: 270.34800
  • Catalog: Apoptosis
  • Density: 1.184g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Alisol F 24-acetate

Alisol F 24-acetate is a triterpene compound that can be isolated from the rhizomes of Alisma orientalis. Alisol F 24-acetate inhibits the secretion of HBV surface antigen HBsAg and HBeAg with IC50 values of 7.7 µM and 5.1 µM. Alisol F 24-acetate has proapoptotic activity and can be used for cancer research[1][2].

  • CAS Number: 443683-76-9
  • MF: C32H50O6
  • MW: 530.736
  • Catalog: HBV
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 634.3±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 195.8±25.0 °C

(−)-Conophylline

Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis[1][2].

  • CAS Number: 142741-24-0
  • MF: C44H50N4O10
  • MW: 794.889
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • 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

MMP-9-IN-4

MMP-9-IN-4 is a MMP-9 inhibitor (IC50: 7.46 nM) that has H-π interactions with MMP-9. MMP-9-IN-4 also inhibits AKT activity (IC50: 8.82 nM). MMP-9-IN-4 shows cell cytotoxicity and induces cell apoptosis. MMP-9-IN-4 can be used in the research of cancers[1].

  • CAS Number: 2581824-39-5
  • MF: C28H19F3N4O6
  • MW: 564.47
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PB 28 dihydrochloride

A potent, mixed sigma2 agonist and sigma1 antagonist with Ki of 0.28 and 13.0 nM, respectively; inhibits cancer cell growth, modulates P-glycoprotein, and synergizes with doxorubicin in MCF7 and MCF ADR cells with IC50 in nanomolar range; increase G0-G1-phase fraction and caspase-independent apoptosis, also reduces P-gp expression.

  • CAS Number: 172907-03-8
  • MF: C24H40Cl2N2O
  • MW: 443.493
  • Catalog: SARS-CoV
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Sandacanol

Sandacanol is a specific agonist of olfactory receptor (OR10H1). Sandacanol induces cell cycle arrest and some apoptosis in bladder cancer cells[1].

  • CAS Number: 28219-61-6
  • MF: C14H24O
  • MW: 208.340
  • Catalog: Apoptosis
  • Density: 0.9±0.1 g/cm3
  • Boiling Point: 287.4±9.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 103.5±15.0 °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

CA3(CIL56)

CIL56 is a potent and selective ferroptosis inducer. Ferroptosis is an iron-dependent form of regulated cell death (RCD).

  • CAS Number: 300802-28-2
  • MF: C23H27N3O5S2
  • MW: 489.608
  • Catalog: Ferroptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 741.7±70.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 402.4±35.7 °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

Acetyl-Neurotrophin Receptor (368-381) amide (human)

NTR 368 is a peptide derived from p75 neurotrophin receptor (p75NTR) corresponding to residues 368-381 of the human receptor. NTR 368 has helix forming propensity in the presence of micellar lipid. NTR 368 is a potent inducer of neural apoptosis[1].

  • CAS Number: 197230-90-3
  • MF: C69H124N22O19
  • MW: 1565.86000
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Adenosine-13C5

Adenosine-13C5 is the 13C labeled Adenosine[1]. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation[2][3].

  • CAS Number: 159496-13-6
  • MF: C10H13N5O4
  • MW: 272.20500
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

AZD5582

AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively). IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]Target: IAPs inhibitorAZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].

  • CAS Number: 1258392-53-8
  • MF: C58H78N8O8
  • MW: 1015.289
  • Catalog: IAP
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1207.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 683.9±34.3 °C

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

Mimosine

Mimosine, a tyrosine analog , can act as an antioxidant by its potent iron-binding activity[1]. Mimosine is a known chelator of Fe(III)[2]. Mimosine induces apoptosis through metal ion chelation, mitochondrial activation and ROS production in human leukemic cells[3]. Anti-cancer, antiinflammation.

  • CAS Number: 500-44-7
  • MF: C8H10N2O4
  • MW: 198.18
  • Catalog: Apoptosis
  • Density: 1.544g/cm3
  • Boiling Point: 428.6ºC at 760mmHg
  • Melting Point: 224-228 °C
  • Flash Point: 213ºC

Eriocalyxin B

Eriocalyxin B is an ent-Kaurene diterpenoid isolated from Chinese herb Isodon eriocalyx. Eriocalyxin B has anti-cancer and anti-infammatory activities. Eriocalyxin B induces cell apoptosis[1].

  • CAS Number: 84745-95-9
  • MF: C20H24O5
  • MW: 344.402
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 551.1±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 198.9±23.6 °C

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

Destruxin B

Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells[1]. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo[2].

  • CAS Number: 2503-26-6
  • MF: C32H55N5O7
  • MW: 593.75500
  • Catalog: Apoptosis
  • Density: 1.17g/cm3
  • Boiling Point: 875ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 483ºC

Mitotane-d8

Mitotane-d8 is the deuterium labeled Mitotane[1]. Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has drug-drug interactions[2][3][4][5].

  • CAS Number: 2673270-14-7
  • MF: C14H2D8Cl4
  • MW: 328.09
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Glutamine-13C5,d5,15N2

L-Glutamine-13C5,d5,15N2 (L-Glutamic acid 5-amide-13C5,d5,15N2) is the deuterium, 13C-, and 15-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: 2123439-02-9
  • MF: 13C5H5D515N2O3
  • MW: 158.13
  • Catalog: Ferroptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Moexipril-d5

Moexipril-d5 is the deuterium labeled Moexipril. Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme(ACE) inhibitor, which is used for the treatment of hypertension and congestive heart failure[1][2].

  • CAS Number: 1356929-49-1
  • MF: C27H29D5N2O7
  • MW: 503.60
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A