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.

 
 
Apoptosis Products New Apoptosis Products Compare Solubility


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Catalog No. Product Name Application Product Information
A13725

10058-F4

c-Myc-Max inhibitor
10058-F4 is a c-Myc inhibitor that prevents c-Myc/Max dimerization.
A16112

A-1155463

BCL-XL inhibitor
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)
A15545

A-1210477

MCL-1 inhibitor
A-1210477 is a potent and selective MCL-1 inhibitor. A-1210477 induces the hallmarks of intrinsic apoptosis and demonstrates single agent killing of multiple myeloma and non-small cell lung cancer cell lines.
A16190

A-1331852

BCL-XL inhibitor
A-1331852 is a potent and BCL-XL-selective inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.
A12500

ABT-199 (Venetoclax)

Bcl-2 inhibitor
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)

Bcl-2 inhibitor
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

Bcl-2 Inhibitor
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

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

Ac-IEPD-AFC

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

Ac-LEHD-AFC

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

Acetate gossypol

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

AMG232

MDM2 inhibitor
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).
A16314

Apogossypolone (ApoG2)

Bcl-2 inhibitor
Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with
A11944

Apoptosis Activator 2

Apoptosis Activator
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.
A13058

Apoptosis Inhibitor (M50054)

Apoptosis Inhibitor
Apoptosis Inhibitor is a cell-permeable inhibitor of apoptosis induction.
A11289

Apremilast (CC 10004)

PDE4 Inhibitor
Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.
A15004

AT-101

Bcl-2 Inhibitor
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 (SM-406, ARRY-334543)

IAP inhibitor
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

pan Bcl-2 inhibitor
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

Caspase-3 inhibitor
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

Bax activator
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.
A13580

Bcl-2 Inhibitor

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

Bcl-2 antagonist
BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.
A16061

BH3I-1

Bcl-XL antagonist
BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL
A12738

Birinapant (TL32711)

XIAP/cIAP1 antagonist
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.

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