Inhibitor SourceBook™ Second Edition
Inhibitor SourceBook™ Second Edition
Inhibitor SourceBook™ Second Edition
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Other Selected <strong>Inhibitor</strong>s of Apoptosis<br />
Calbiochem • <strong>Inhibitor</strong> SourceBook<br />
Apoptosis<br />
Product Cat. No. Comments Size Price<br />
Apoptosis <strong>Inhibitor</strong> 178488 [M50054; 2,2´-Methylenebis(1,3-cyclohexanedione)]<br />
A cell-permeable inhibitor of apoptosis induction (IC 50 = 283 mM in FasL-stimulated<br />
WC8 cells, 550 mM in etoposide-stimulated U937 cells). The anti-apoptotic effects<br />
are attributed to the inhibition of caspase-3 activation (IC 50 = 334 mM in etoposidestimulated<br />
U937 cells).<br />
Apoptosis <strong>Inhibitor</strong> II,<br />
NS3694<br />
178494 (NS3694)<br />
A cell-permeable compound that specifically prevents the active ~700 kDa apoptosome<br />
complex formation triggered by cytochrome c release. Protects against apoptosomemediated<br />
caspase activation and cell death.<br />
Bax Channel Blocker 196805 [(±)-1-(3,6-Dibromocarbazol-9-yl)-3-piperazin-1-yl-propan-2-ol, bis TFA]<br />
A cell-permeable dibromocarbazolo-piperazinyl derivative that displays anti-apoptotic<br />
properties. Effectively blocks Bid-induced cyctochrome c release from HeLa cell<br />
mitochondria (~80% inhibition at 5 mM) by inhibiting Bax channel-forming activity<br />
(IC 50 = 520 nM in a liposome channel assay).<br />
Bax-Inhibiting Peptide,<br />
V5<br />
Bax-Inhibiting Peptide,<br />
Negative Control<br />
Fas/FasL Antagonist,<br />
Kp7-6<br />
Humanin, Human,<br />
Synthetic<br />
Omi/HtrA2 Protease<br />
<strong>Inhibitor</strong>, Ucf- 0<br />
196810 (BIP-V5; H-VPMLK-OH)<br />
A cell-permeable pentapeptide based on the Ku70-Bax inhibiting domain that offers<br />
cytoprotection. Functions as effectively as the Caspase <strong>Inhibitor</strong> VI (Z-VAD-FMK; Cat.<br />
No. 2 9007) for Bax-mediated apoptosis (~50–200 mM).<br />
196811 (BIP-NC; H-IPMIK-OH)<br />
A cell-permeable mutated analog of the Bax-Inhibiting Peptide, V5 (Cat. No. 968 0)<br />
that serves as a negative control. Does not suppress Bax-mediated apoptosis (~200 mM).<br />
341291 (H-YC*DEHFC*Y-OH, Cyclic [Cys-Cys disulfide]; Kp7-6)<br />
Specifically antagonizes Fas/FasL-mediated cellular apoptotic signals (58% reduction<br />
of FasL-induced apoptosis in Jurkat cells at mg/ml). Binds to FasL (Cat. Nos. PF033<br />
and PF092) and Fas (CD95/APO- ) with comparable affinity (K = .2 and 3.2 mM,<br />
d<br />
respectively).<br />
400140 (H-MAPRGFSCLLLLTSEIDLPVKRRA-OH; HN)<br />
An anti-apoptotic peptide that when expressed intracellularly, offers protection against<br />
neuronal apoptosis induced by presenilin and APP mutants associated with familial<br />
Alzheimer’s disease (AD). Reduces cytochrome c release in vitro by directly binding to Bax<br />
(K ~2 nM).<br />
d<br />
496150 {High Temperature Requirement A2 <strong>Inhibitor</strong> I; 5-[5-(2-Nitrophenyl)furfurylidine]-1,3diphenyl-2-thiobarbituric<br />
Acid}<br />
A cell-permeable furfurylidine-thiobarbituric acid compound that acts as a potent,<br />
specific, competitive, and reversible inhibitor of the pro-apoptotic, heat-inducible,<br />
mitochondrial serine protease Omi/HtrA2 (IC = 9.5 mM for His-Omi ). Shows very<br />
50 34-458<br />
little activity against various other serine proteases tested (IC ≥ 200 mM). Reported to<br />
50<br />
block Omi/HtrA2 induced cell death in caspase-9 (-/-) null fibroblasts.<br />
Pifithrin-a 506132 [2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone, HBr]<br />
A cell-permeable chemical inhibitor of p53. Reversibly inhibits p53-dependent<br />
transactivation of p53-responsive genes and reversibly blocks p53-mediated apoptosis.<br />
Pifithrin-a, Cyclic- 506134 {2-(4-Methylphenyl)imidazo[2,1-b]-5,6,7,8-tetrahydrobenzothiazole, HBr; QB102}<br />
A cell-permeable and very stable analog of Pifithrin-a (Cat. No. 506 32) with similar<br />
biological functions, but with reduced cytotoxicity. Reversibly blocks p53-mediated<br />
apoptosis.<br />
0 mg $96<br />
0 mg $ 00<br />
5 mg $84<br />
5 mg $84<br />
5 mg $84<br />
25 mg $237<br />
mg $252<br />
0 mg $98<br />
5 mg<br />
0 mg<br />
$65<br />
$ 2<br />
0 mg $ 27<br />
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