Apoptosis

The process of programmed cell death (PCD), or apoptosis, is generally characterized by distinct morphological characteristics and energy-dependent biochemical mechanisms. Apoptosis is considered a vital component of various processes including normal cell turnover, proper development and functioning of the immune system, hormone-dependent atrophy, embryonic development and chemical-induced cell death. Inappropriate apoptosis (either too little or too much) is a factor in many human conditions including neurodegenerative diseases, ischemic damage, autoimmune disorders and many types of cancer. 

The mechanisms of apoptosis are highly complex and sophisticated, involving an energy-dependent cascade of molecular events. To date, research indicates that there are two main apoptotic pathways: the extrinsic or death receptor pathway and the intrinsic or mitochondrial pathway. However, there is now evidence that the two pathways are linked and that molecules in one pathway can influence the other.

 There are many pathological conditions that feature excessive apoptosis and thus may benefit from artificially inhibiting 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 polymerase) inhibition, stimulation of the PKB/Akt (protein kinase B) pathway, and inhibition of Bcl-2 proteins. So far, members of the IAP family have been investigated as therapeutic targets for the treatment of stroke, spinal cord injuries, multiple sclerosis as well as cancer. The synthetic nonspecific caspase inhibitor z-VAD-fmk was shown to reduce the severity of myocardial reperfusion injury in rat and mouse models of myocardial infarction. Specific inhibitors of caspase activity may also prove beneficial.

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Category
  1. Bcl-2 Family (16)
  2. Caspase (25)
  3. p53 (19)
  4. TNF-α (4)
  5. IAP (4)
  6. RasGAP (Ras- P21) (4)
  7. MDM2 (13)
  8. Apoptosis Inducers (5)
  9. PERK (3)
Target
  1. Bcl-2 (9)
  2. Bcl-w (2)
  3. Bcl-xL (5)
  4. Mcl-1 (3)
Actions
  1. Activator (15)
  2. Antagonist (3)
  3. Inducer (2)
  4. Inhibitor (55)
  5. Substrate (2)
 
 
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Catalog No. Product Name Product Information
A16112

A-1155463

A-1155463 is a highly potent and selective BCL-XL inhibitor, A-1155463 shows picomolar binding affinity to BCL-XL (Ki ??0.01 nM), and >1000-fold weaker binding to BCL-2 (Ki = 80 nM) and related proteins BCL-W (Ki = 19 nM) and MCL-1 (Ki > 440 nM)
A12500

ABT-199 (Venetoclax)

ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.
A10022

ABT-263 (Navitoclax)

ABT-263 (Navitoclax) is a potent orally bioavailable SMI that is structurally related to ABT-737. ABT-263 disrupts Bcl-2 - Bcl-XL interactions with pro-apoptotic proteins .
A10255

ABT-737

ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).
A15816

Ac-DEVD-CHO

Ac-DEVD-CHO is an aldehyde peptide and a CPP32/Apopain Inhibitor.
A15319

Ac-IEPD-AFC

Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9.
A15291

Ac-LEHD-AFC

Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC.
A14795

Acetate gossypol

Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic.
A14394

AMG232

AMG 232 is a highly potent, selective and orally bioavailable piperidinone inhibitor of the MDM2-p53 interaction((SPR KD= 0.045 nM, SJSA-1 EdU IC50=9.1 nM).
A11944

Apoptosis Activator 2

Apoptosis Activator 2 activates caspases in a cytochrome c-dependent manner and induces apoptosis in tumor cells by promoting the oligomerization of Apaf-1 into the mature apoptosome.
A15004

AT-101

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM.
A11163

AT-406

AT-406 is an orally bioavailable inhibitor of IAP family of proteins with potential apoptotic inducing and antineoplastic activity. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP).
A13578

AT101 acetic acid

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID
A15294

AZ 10417808

AZ 10417808, selective non-peptide inhibitor of caspase-3 (Ki = 247 nM); displays > 40-fold selectivity over caspases 1, 2, 6, 7 and 8 (Ki > 10 ??M).
A12907

BAM 7

BAM 7 binds the BAX trigger site with an EC50 ~ 3.3 μM as measured in a competitive FP assay using FITC-BIM SAHB and BAX.
A11957

Bay 11-7821

Bay 11-7821 is an irreversible inhibitor of TNF-α-stimulated IκBα phosphorylation.
A13580

Bcl-2 Inhibitor

Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-x in vitro (IC50 =10 uM and 7 uM, respectively).
A15821

BDA-366

BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.
A12738

Birinapant (TL32711)

Birinapant, also known as TL32711, is a synthetic small molecule and peptido mimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.
A12743

BM-1074

BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM.
A15392

Boc-D-FMK

BOC-D-FMK is a Novel inhibitor of Caspase-3.
A14919

Caspase-3/7 Inhibitor I

Caspase-3/7 Inhibitor I is a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM).
A11635

Cyclophosphamide monohydrate

Cyclophosphamide monohydrate is an alkylating, cytotoxic agent experimentally shown to crosslink DNA, causing strand breakage and inducing mutations.
A11394

Emricasan

Emricasan is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases.
A11279

FK866

FK866, a highly specific noncompetitive inhibitor of nicotinamide phosphoribosyltransferase, represents a novel mechanism for induction of tumor cell apoptosis.

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