476495

PKD Inhibitor, CID755673

The PKD Inhibitor, CID755673, also referenced under CAS 521937-07-5, controls the biological activity of PKD. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonim(y): PKD Inhibitor, CID755673, 7-Hydroxy-2,3,4,5-tetrahydro-1H-[1]benzofuro[2,3-c]azepin-1-one, PKCμ Inhibitor
• Wzór empiryczny (zapis Hilla): C₁₂H₁₁NO₃
• Numer CAS: 521937-07-5
• Masa cząsteczkowa: 217.22
• Numer MDL: MFCD03828155
• Kod UNSPSC: 12352200
• NACRES: NA.28

Właściwości

• Poziom jakości: 100
• Próba: ≥95% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: brown
• rozpuszczalność: DMSO: 50 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 2-8°C
• InChI: 1S/C12H11NO3/c14-7-3-4-10-9(6-7)8-2-1-5-13-12(15)11(8)16-10/h3-4,6,14H,1-2,5H2,(H,13,15)
• Klucz InChI: AACFPJSJOWQNBN-UHFFFAOYSA-N

Opis

Opis ogólny

A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ isoforms 1, 2, & 3 (IC₅₀ = 182, 280, and 227 nM, respectively), while exhibiting ≥30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIα, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µM, including Akt1/2 and PKCα/β/δ/ζ. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser⁷⁴² and Ser⁹¹⁶ in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3β, CKIδ, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µM inhibitor = 95, 86, 82, 75, 71, and 50, respectively).

A cell-permeable benzoxoloazepinolone compound that effectively inhibits syntide-2 (Cat. No. 05-23-4910) phosphorylation by all three PKD/PKCµ isoforms 1, 2, & 3 (IC₅₀ = 182, 280, and 227 nM, respectively), while exhibiting ≥30-fold less potency towards Cdk activating kinase, Plk1, CaMKIIα, as well as 44 other kinases, 33 of which are not significantly inhibited even at concentrations as high as 10 µM, including Akt1/2 and PKCα/β/δ/ζ. Shown to block PMA- (Cat. No. 524400) induced PKD1 phosphorylation on Ser⁷⁴² and Ser⁹¹⁶ in LNCaP cells, PMA-induced HCAS5 nuclear export in HeLa cells, as well as other PKD-mediated cellular responses. The mode of inhibition is demonstrated not to be ATP-competitive in nature. Also reported to inhibit MAPKAPK2, GSK-3β, CKIδ, MK5 (PRAK), CDK2, and Erk1 kinase activity at much elevated concentrations (% inhibition by 10 µM inhibitor = 95, 86, 82, 75, 71, and 50, respectively).

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 3 months at -20°C.

Inne uwagi

LaValle, C.R., et al. 2010. BMC Chemical Biology10, 5.
Sharlow, E.R., et al. 2008. J. Biol. Chem.283, 33516.

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 3