513022

PD 150606

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 and 370 nM for calpain-2.

• Synonim(y): Kwas 3-(4-jodofenylo)-2-merkapto-(Z)-2-propenowy
• Wzór empiryczny (zapis Hilla): C₉H₇IO₂S
• Numer CAS: 426821-41-2
• Masa cząsteczkowa: 306.12
• Numer MDL: MFCD00011966
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: off-white
• rozpuszczalność: DMSO: 100 mg/mL; methanol: 25 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: −20°C

Opis

Opis ogólny

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 (Cat. Nos. 208712 and 208713) and 370 nM for calpain-2 (Cat. Nos. 208715 and 208718)] directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and cathepsin L. Does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis in thymocytes.

A cell-permeable, selective non-peptide calpain inhibitor (K_i = 210 nM for calpain I and 370 nM for calpain II) directed towards the calcium- binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and L. PD 150606 is a non-competitive inhibitor with respect to the substrate and does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis of thymocytes.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
Calpain-1

Product does not compete with ATP.

Reversible: no

Target K_i: 210 nM for calpain-1 and 370 nM for calpain-2

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Inne uwagi

Lin, G.D., et al. 1997. Nat. Struct. Biol. 4, 539.
Squier, M.K., and Cohen, J.J. 1997. J. Immunol. 158, 3960.
Edelstein, C.L., et al. 1996. Kidney Int. 50, 1150.
Wang, K.K.W., et al. 1996. Proc. Natl. Acad. Sci. USA 93, 6687.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 1
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable