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
A12907 SALE

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.
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
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-XL in vitro (IC50 =10 uM and 7 uM, respectively).
A14795

Acetate gossypol

Bcl-2 Inhibitor
Acetate gossypol, a polyphenolic compound isolated from cottonseeds, inhibits Bcl-2 by acting as a BH3 mimetic.
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)
A16061 SALE

BH3I-1

Bcl-XL antagonist
BH3I-1 is a cell permeable BH3 mimetic that binds to Bcl-xL
A15821

BDA-366

Bcl-2 antagonist
BDA-366 selectively inhibits BCL2, converting it to a cell death inducer.
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.
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.
A16190

A-1331852

BCL-XL inhibitor
A-1331852 is a potent and selective BCL-XL inhibitor. BCL-XL is the major antiapoptotic survival protein and may be a novel therapeutic target in CML.
A16192

CID5721353

BCL6 inhibitor
CID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).
A13327

WEHI-539 hydrochloride

Bcl-xL inhibitor
WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM [1].
A16314

Apogossypolone (ApoG2)

Bcl-2 inhibitor
Apogossypolone is a nonpeptidic small-molecule inhibitor of Bcl-2 with
A16315

MIM1

Mcl-1 inhibitor
MIM1 is a selective small molecule inhibitor of Mcl-1(IC50= 4.8 μM) that overcomes Mcl-1-dependent leukemia cell survival.
A16316

(+)-Apogossypol

Bcl-2 family inhibitor
(+)-Apogossypol is a potent inhibitor of Bcl-2 family proteins; competing with the BH3 peptide-binding sites on Bcl-2, Bcl-XL, Mcl-1, Bcl-W, and Bcl-B, but not Bfl-1, with IC50s of 0.5 to 2 μM.
A16323

(S)-Gossypol acetic acid

Bcl-2 inhibitor
(S)-Gossypol acetic acid is a inhibitor of Bcl-2, potently induce cell death in Jurkat cells overexpressing Bcl-2 (IC50, 18.1μM) or Bcl-xL (IC50, 22.9μM).
A16380

Pyridoclax

Mcl-1 inhibitor
Pyridoclax is a potent Mcl-1 inhibitor with Kd value of 25 nM.
A15340

Muristerone A

EcR agonist
Muristerone A is a phytoecdysteroid analog of ecdysone which induces genes in mammalian cells and causes apoptosis in cells transfected with wild-type Bax.
A15338

Bax inhibitor peptide, negative control

Bax inhibitor
Bax inhibitor peptide, negative control, negative control peptide for the Bax inhibitor peptides V5 and P5 , which inhibit Bax translocation to mitochondria and Bax-mediated apoptosis in vitro.
A10255 SALE

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).
A10022 SALE

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 .
A10665 SALE

Obatoclax mesylate (GX15-070)

Bcl-2 Inhibitor
Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).
A10955

TW-37

Bcl-2 inhibitor
TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1.
A11448 SALE

HA14-1

Bcl-2 inhibitor
HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2.
A11988 SALE

Gambogic acid

Bcl-2 inhibitor
Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.
A12743

BM-1074

Bcl-2/Bcl-xL inhibitor
BM-1074 is a potent and efficacious Bcl-2/Bcl-xL inhibitor with Ki of <1 nM.
A12823

Sabutoclax

Bcl-2 inhibitor
Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
A12500 SALE

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.
A14222 SALE

UMI-77

Mcl-1 inhibitor
UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.
A15335

Bax channel blocker

Bax channel blocker
Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome C release (IC50 = 0.52 μM).
A15336

Bax inhibitor peptide P5

Bax inhibitor
Bax inhibitor peptide P5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.
A15337 SALE

Bax inhibitor peptide V5

Bax inhibitor
Bax inhibitor peptide V5, cell-permeable synthetic peptide inhibitor of Bax translocation to mitochondria; designed from Ku70, a protein that is suggested to suppress the mitochondrial translocation of Bax. Inhibits Bax-mediated apoptosis in vitro.
A15308

PETCM

Caspase-3 activator
PETCM is an activator of caspase-3 and a stimulator of apoptosome formation in HeLa cell cytosols.
A15319

Ac-IEPD-AFC

Fluorogenic caspase substrate
Ac-LEHD-AFC is a fluorogenic substrate for caspase-4, caspase-5, and caspase-9.
A15816

Ac-DEVD-CHO

Caspase Inhibitor
Ac-DEVD-CHO is an aldehyde peptide and a CPP32/Apopain Inhibitor.
A12611

Z-VEID-FMK

Caspase-6 inhibitor
Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2.
A12637

Z-VDVAD-FMK

Caspase-2 inhibitor
Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes.
A12697

Z-DQMD-FMK

Caspase-3 inhibitor
Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.
A12800

Z-IETD-FMK

caspase 8 inhibitor
Z-IETD-FMK is a specific inhibitor of caspase 8.
A15300

Ivachtin

Caspase-3 inhibitor
Ivachtin is a potent, cell-permeable, reversible, non-competitive inhibitor of Caspase-3 (IC50 = 23 nM).
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 uM).
A15291

Ac-LEHD-AFC

Fluorogenic caspase substrate
Ac-LEHD-AFC, fluorogenic caspase substrate. Analog of the caspase-9 substrate, LEHD-AFC.
A12373 SALE

Z-VAD-FMK

Pan Caspase Inhibitor
Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.
A14100

Nivocasan (GS-9450)

Caspase inhibitor
Nivocasan is a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis/apoptosis animal models.
A13503 SALE

Z-DEVD-FMK

Caspase-3 Inhibitor
Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.
A14358

Z-LEHD-FMK

Caspase-9 Inhibitor
Z-LEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-9 and related caspase activity.
A14915 SALE

Q-VD-OPh hydrate

Caspase inhibitor
Q-VD-OPH is a selective, brain and cell permeable, highly potent and irreversible inhibitor of caspase-3 ( IC50=25nm), caspase-1 (IC50=50nM), caspase-8 (IC50=100nM) and caspase-9 (IC50=430nM).
A14916

Z-WEHD-FMK

Caspase inhibitor
Z-WEHD-FMK is a synthetic peptide that irreversibly inhibits caspase-5 and related caspase activity.
A14919

Caspase-3/7 Inhibitor I

Caspase-3/7 Inhibitor
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).
A16381

Z-FA-FMK

Cysteine protease inhibitor
Z-FA-FMK is an irreversible inhibitor of cysteine protease

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