[CAS NO. 1438881-19-6] CRT0066854

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PRODUCTS SPECIFICATIONS [1438881-19-6]

Catalog

HY-18713

Brand

MCE

CAS

1438881-19-6

DESCRIPTION [1438881-19-6]

Overview

MDL	-
Molecular Weight	415.55
Molecular Formula	C24H25N5S
SMILES	N[C@H](CNC1=NC(C2=CC=NC=C2)=NC3=C1C(CCCC4)=C4S3)CC5=CC=CC=C5

For research use only. We do not sell to patients.

Summary

CRT0066854 is a potent and selective atypical PKC isoenzymes inhibitor. CRT0066854 is against full-length (FL) PKCι , PKCζ , and ROCK-II kinases with IC ₅₀ values of 132 nM, 639 nM, and 620 nM, respectively ^[1] .

IC50 & Target

PKCζ

639 nM (IC ₅₀ )

ROCK2

620 nM (IC ₅₀ )

In Vitro

CRT0066854 displaces a crucial Asn-Phe-Asp motif that is part of the adenosine-binding pocket and engages an acidic patch used by arginine-rich PKC substrates ^[1] .
CRT0066854 (0.2-1.2 μM; 6 days) is able to restore polarized morphogenesis in the dysplastic H-Ras spheroids, and the maximal proportion of spheroids with PSALs is at the lower dose of 1.2 μM ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 120.32 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4064 mL	12.0322 mL	24.0645 mL
5 mM	0.4813 mL	2.4064 mL	4.8129 mL
10 mM	0.2406 mL	1.2032 mL	2.4064 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Kjær S, et al. Adenosine-binding motif mimicry and cellular effects of a thieno[2,3-d]pyrimidine-based chemical inhibitor of atypical protein kinase C isoenzymes. Biochem J. 2013 Apr 15;451(2):329-42.