CRT0066854 hydrochloride

SKU: orb1709980

Description

CRT0066854 hydrochloride is a selective atypical PKC inhibitor, demonstrating potent activity against PKCι, PKCζ, and ROCK-II with IC50 values of 132 nM, 639 nM, and 620 nM, respectively. This compound is a valuable research tool for investigating PKC signaling in cancer biology and other disease models, with utility in both in vitro and in vivo studies.

Research Area

Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 2250019-91-9
• MW: 488.48
• Purity: 99.63% (May vary between batches)
• Formula: C₂₄H₂₇Cl₂N₅S
• SMILES: N[C@@H](CC1=CC=CC=C1)CNC2=C3C4=C(CCCC4)SC3=NC(C5=CC=NC=C5)=N2.Cl.Cl
• Target: PKC,ROCK
• Solubility: DMSO:45 mg/mL (92.12 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (10.24 mM)

Bioactivity

• Target IC50:
  ROCK2:620 nM|PKCζ:639 nM
• In Vitro:
  CRT0066854 hydrochloride replaces the crucial Asn-Phe-Asp motif, which is part of the adenosine binding pocket and joins with the acidic patch used by the PKC substrate rich in arginine. CRT0066854 hydrochloric acid Salt (0.2-1.2μM; 6 days) can restore polarized morphogenesis. Among the dysplastic H-Ras spheroids, the maximum proportion of PSAL spheroids was 1.2 μM at a lower dose.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CRT-0066854 Hydrochloride, CRT-0066854 hydrochloride, CRT 0066854 Hydrochloride, CRT0066854 Hydrochloride, CRT0066854 hydrochloride, ROCK2, ROCKII, PKCζ

Compound Identifiers

PubChem CID

131954580