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.


Anti-infection >
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Antibody-drug Conjugate >
ADC Cytotoxin ADC Linker Drug-Linker Conjugates for ADC PROTAC-linker Conjugate for PAC
Apoptosis >
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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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Tanshinone IIB

Tanshinone IIB is a major active constituent of the roots of Salvia miltiorrhiza (Danshen) widely used for the research of stroke and coronary heart disease in Asian countries. Tanshinone IIB has a neuroprotective effect via inhibition of apoptosis[1].

  • CAS Number: 17397-93-2
  • MF: C19H18O4
  • MW: 310.344
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 536.9±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 278.5±30.1 °C

FLUNISOLIDE

Flunisolide hemihydrate is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide hemihydrate can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation[1][2].

  • CAS Number: 77326-96-6
  • MF: C48H64F2O13
  • MW: 887.01100
  • Catalog: Apoptosis
  • Density: 1.33 g/cm3
  • Boiling Point: 581.8ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 305.7ºC

β-Apopicropodophyllin

β-Apopicropodophyllin is a nature product that could be isolated from Hyptis wticillata.β-Apopicropodophyllin induces apoptosis by inducing microtubule disruption, DNA damage, cell cycle arrest and ER stress. β-Apopicropodophyllin can be used in research of cancer[1].

  • CAS Number: 477-52-1
  • MF: C22H20O7
  • MW: 396.39000
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

10-Formyl-5,8-dideazafolic acid

10-Formyl-5,8-dideazafolic acid is a thymidylate synthase inhibitor[1].

  • CAS Number: 61038-31-1
  • MF: C22H21N5O7
  • MW: 467.43100
  • Catalog: Thymidylate Synthase
  • Density: 1.54g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-Hydroxybakuchiol

3-Hydroxybakuchiol can be isolated from Otholobium mexicanum J. W. Grimes. 3-Hydroxybakuchiol is an electron transport chain (ETC) inhibitor. 3-Hydroxybakuchiol has antitumor activity, and induces tumor cell apoptosis. 3-Hydroxybakuchiol also has moderate inhibitory activity against α-glucosidase (IC50: 345 μM)[1][2].

  • CAS Number: 178765-54-3
  • MF: C18H24O2
  • MW: 272.382
  • Catalog: Apoptosis
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 437.6±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 200.4±23.3 °C

TMCB

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].

  • CAS Number: 1085822-09-8
  • MF: C11H9Br4N3O2
  • MW: 534.82
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Isosilybin A

Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis[1][2].

  • CAS Number: 142796-21-2
  • MF: C25H22O10
  • MW: 482.43600
  • Catalog: Apoptosis
  • Density: 1.527±0.06 g/cm3
  • Boiling Point: 793.0±60.0 °C(Predicted)
  • Melting Point: 201-203 ºC (methanol water )
  • Flash Point: N/A

Etoposide 4'-Phosphate

Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy[1][2].

  • CAS Number: 117091-64-2
  • MF: C29H33O16P
  • MW: 666.522
  • Catalog: Apoptosis
  • Density: 1.55 g/cm3
  • Boiling Point: 907.7±75.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 502.7±37.1 °C

Cucurbitacin IIB

Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α[1].

  • CAS Number: 50298-90-3
  • MF: C30H48O7
  • MW: 520.698
  • Catalog: Apoptosis
  • Density: 1.22±0.1 g/cm3
  • Boiling Point: 668.4±55.0 °C at 760 mmHg
  • Melting Point: 158-159ºC
  • Flash Point: 372.0±28.0 °C

Necrostatin 2 (S enantiomer)

Necrostatin 2 is a potent necroptosis inhibitor with EC50 of 50 nM.IC50 Value: 50 nM (EC50) [1]Target: TNF-alphaNecrostatin 2 is a potent in vitro necroptosis inhibitors (exemplified by 1, EC50-0.05 uM) that also were efficacious in an animal model of ischemic stroke. Many Necroptosis inhibitor derivatives are designed for researchers.Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling necrosis. It can be induced in a FADD-deficient variant of human Jurkat T cells treated with TNF-a. 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1H-indol-3-ylmethyl)hydantoins were found to be potent necroptosis inhibitors (called necrostatins).

  • CAS Number: 852391-20-9
  • MF: C13H12ClN3O2
  • MW: 277.70600
  • Catalog: TNF Receptor
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HJC0416 hydrochloride

HJC0416 hydrochloride is a potent and orally active STAT3 inhibitor with an enhanced anticancer profile than Stattic (HY-13818). HJC0416 hydrochloride is a promising anti-cancer agent for breast cancer study[1].

  • CAS Number: 2415263-08-8
  • MF: C18H18Cl2N2O4S
  • MW: 429.32
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Obatoclax (GX15-070)

Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2[1][2]. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity[3][4].

  • CAS Number: 803712-67-6
  • MF: C20H19N3O
  • MW: 317.384
  • Catalog: Bcl-2 Family
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 570.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 298.8±30.1 °C

AM-8553

A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM; exhibits excellent pharmacokinetic properties and in vivo efficacy.

  • CAS Number: 1352064-70-0
  • MF: C25H29Cl2NO4
  • MW: 478.408
  • Catalog: MDM-2/p53
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 644.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 343.3±31.5 °C

PCC0208017

PCC0208017 is a microtubule affinity regulating kinases (MARK3/MARK4) inhibitor with IC50s of 1.8 and 2.01 nM, respectively. PCC0208017 has much lower inhibitory activity against MARK1 and MARK2, with IC50s of 31.4 and 33.7 nM, respectively. PCC0208017 suppresses glioma progression in vitro and in vivo. PCC0208017 disrupts microtubule dynamics and induces G2/M phase cell cycle arrest and cell apoptosis. PCC0208017 demonstrates robust antitumor activity in vivo and displays good BBB permeability[1].

  • CAS Number: 2623158-64-3
  • MF: C19H20F3N7
  • MW: 403.40
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Prosapogenin A

Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis[1].

  • CAS Number: 19057-67-1
  • MF: C39H62O12
  • MW: 722.902
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 838.8±65.0 °C at 760 mmHg
  • Melting Point: 212℃
  • Flash Point: 461.1±34.3 °C

PK095

PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer[1].

  • CAS Number: 380314-37-4
  • MF: C20H18N4O2S
  • MW: 378.45
  • Catalog: MDM-2/p53
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Rosamultic acid

Rosamultic acid is an A-ring contracted triterpene, that can be isolated from the roots of Rosa rnultiflora. Rosamultic acid inhibits gastric cancer cells proliferation by inducing Apoptosis mediated through cell cycle arrest, downregulation of cell cycle related protein expressions, inhibition of cell migration, DNA damage, and activation of caspases[1][2].

  • CAS Number: 214285-76-4
  • MF: C30H46O5
  • MW: 486.683
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 630.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 348.9±28.0 °C

Z-IETD-pNA

Z-IETD-pNA (Z-Ile-Glu-Thr-Asp-pNA) is a colorimetric caspase-8 and granzyme B substrate. Z-IETD-pNA is hydrlyzed by caspase 8 to generate pNA[1].

  • CAS Number: 348079-18-5
  • MF: C33H42N6O13
  • MW: 730.72
  • Catalog: Caspase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

VEGFR-2-IN-22

VEGFR-2-IN-22 (Compound 25) is a dual VEGFR-2 and β-tubulin polymerization inhibitor with an IC50 of 19.82 nM against VEGFR-2. VEGFR-2-IN-22 induces apoptosis[1].

  • CAS Number: 2447587-73-5
  • MF: C26H24ClFN4O6
  • MW: 542.94
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bcl-2-IN-10

Bcl-2-IN-10 is an active Bcl-2 inhibitor that can release up to four nitric oxide (NO) molecules. Bcl-2-IN-10 has cytotoxic activities against cancer cells, such as human leukemia, breast cancer and lung cancer. Bcl-2-IN-10 induces cell apopotosis and arrest cell cycle of G2/M phase, and can be used in cancer-related research[1].

  • CAS Number: 2773354-28-0
  • MF: C22H25N11O12
  • MW: 635.50
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

R 7050

R-7050 is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.

  • CAS Number: 303997-35-5
  • MF: C16H8ClF3N4S
  • MW: 380.775
  • Catalog: TNF Receptor
  • Density: 1.6±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Genistein

Genistein, a soy isoflavone, is a multiple tyrosine kinases inhibitor which acts as a chemotherapeutic agent against different types of cancer, mainly by altering apoptosis, the cell cycle, and angiogenesis and inhibiting metastasis.

  • CAS Number: 446-72-0
  • MF: C15H10O5
  • MW: 270.237
  • Catalog: Apoptosis
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 555.5±50.0 °C at 760 mmHg
  • Melting Point: 297-298 °C
  • Flash Point: 217.1±23.6 °C

Obacunone

Obacunone, isolated from seeds of Marsh White grapefruit, exhibits anti-tumor activity by the induction of apoptosis[1].

  • CAS Number: 751-03-1
  • MF: C26H30O7
  • MW: 454.512
  • Catalog: Apoptosis
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 626.2±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 332.5±31.5 °C

Ilexsaponin A

Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes[1].

  • CAS Number: 108524-93-2
  • MF: C36H56O11
  • MW: 664.823
  • Catalog: Apoptosis
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 788.1±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 240.1±26.4 °C

Garivulimab

Garivulimab (BGB-A333) is a humanized IgG1-variant monoclonal antibody that specifically targets and binds to PD-L1. Garivulimab selectively blocks the interaction of PD-L1 and PD-1. Garivulimab has antitumor activity[1].

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

ALK/EGFR-IN-1

ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research[1].

  • CAS Number: 2730430-08-5
  • MF: C27H34ClN7O3S
  • MW: 572.12
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YS-363

YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis[1].

  • CAS Number: 2470908-90-6
  • MF: C30H30N4O3
  • MW: 494.58
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BTM-3528

BTM-3528 is an activator of the mitochondrial protease OMA1 and mediates excessive activation of the mitochondrial integrated stress response (ISR). BTM-3528 stimulates OMA1-dependent DELE1 and OPA1 cleavage and mitochondrial fragmentation. BTM-3528 activates eIF2α kinase HRI, inducing cell growth arrest and apoptosis. BTM-3528 has anticancer activity against multiple DLBCL cell lines and has in vivo inhibitory potency in a mouse model xenografted with human DLBCL SU-DHL-10 cells[1].

  • CAS Number: 2054998-45-5
  • MF: C24H19F4N3O2S2
  • MW: 521.55
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Methoxyestradiol-d5

2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa[1][2][3][4][5][6][7].

  • CAS Number: 358731-34-7
  • MF: C19H21D5O3
  • MW: 307.44
  • Catalog: Apoptosis
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 464.4±45.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 234.7±28.7 °C

SKI-178

SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both drug sensitive and multi-drug resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines[1][2].

  • CAS Number: 1259484-97-3
  • MF: C21H22N4O4
  • MW: 394.42400
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A