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Merck

662125

Ubiquitin Isopeptidase Inhibitor I, G5

The Ubiquitin Isopeptidase Inhibitor I, G5, also referenced under CAS 108477-18-5, controls the biological activity of Ubiquitin Isopeptidase. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

동의어(들):

Ubiquitin Isopeptidase Inhibitor I, G5, 3,5-bis((4-Nitrophenyl)methylene)-1,1-dioxide, tetrahydro-4H-thiopyran-4-one, NSC-144303

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제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C19H14N2O7S
CAS 번호:
Molecular Weight:
414.39
MDL number:
NACRES:
NA.54
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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Quality Segment

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

storage temp.

2-8°C

General description

A cell-permeable cross-conjugated α,β-unsaturated dienone compound that induces caspase activation and apoptosis (IC50 = 1.76 and 1.6 µM in E1A and E1A/C9DN cells, respectively) via the apoptosome-independent mitochondrial pathway by selectively inhibiting ubiquitin isopeptidase activity (IC50 = ~ 30 µM). The cellular expression of Bax and Bak is essential for G5-activated apoptosis, while Bcl-2 appears to protect cells against the effect of G5. G5 is more potent than, but otherwise exhibits similar pharmacological effects as, Ubiquitin Isopeptidase Inhibitor II, F6 (Cat. No. 662126). At higher concentrations (5-10 µM), shown to induce necrosis in apoptosis-resistant MEFs-DKO.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Ubiquitin isopeptidase activity
Product does not compete with ATP.
Reversible: no
Target IC50: ~ 30 µM against ubiquitin isopeptidase activity; 1.76 and 1.6 µM for the induction of caspase activation and apoptosis in E1A and E1A/C9DN cells, respectively

Packaging

Packaged under inert gas

Preparation Note

Unstable in DMSO; reconstitute just prior to use.

Other Notes

Fontanini, A., et al. 2009. J. Biol. Chem.284, 8369.
Aleo, E., et al. 2006. Cancer Res.66, 9235.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Irritant (B)


저장 등급

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable



시험 성적서(COA)

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