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CRT0066854

رقم الكتالوجGC45414

CRT0066854 هو مثبط قوي و انتقائي غير نمطي لإنزيمات PKC

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CRT0066854 التركيب الكيميائي

Cas No.: 1438881-19-6

الحجم السعر المخزون الكميّة
1mg
37٫00
متوفر
5mg
148٫00
متوفر
10mg
241٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of CRT0066854

CRT0066854 is an inhibitor of PKCΙ and PKCζ (IC50s = 132 and 639 nM, respectively).1 It also inhibits the Rho-associated kinase II (ROCK-II) kinase domain (IC50 = 620 nM). It is selective for these atypical PKCs and ROCK-II over typical PKCs and 98 other kinases in a panel at 1 μM. CRT0066854 decreases phosphorylation of the atypical PKC substrate lethal giant larvae 2 (LLGL2) in HEK293 cells expressing PKCΙ and LLGL2. It decreases viability of A549 lung carcinoma cells (IC50 = 3.47 μM) and decreases colony formation in HeLa cells by 65% when used at a concentration of 1 μM. CRT0066854 impairs lumen formation in MDCK cells in a Matrigel• assay and migration of NRK-49F cells in a wound assay.

References
1. Kj•r, S., Linch, M., Purkiss, A., 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. 451(2), 329-342 (2013).

Chemical Properties of CRT0066854

Cas No. 1438881-19-6 SDF
Canonical SMILES N[C@@H](CC1=CC=CC=C1)CNC2=C3C(SC4=C3CCCC4)=NC(C5=CC=NC=C5)=N2
Formula C24H25N5S M.Wt 415.6
الذوبان DMSO: 30 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of CRT0066854

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.4062 mL 12.0308 mL 24.0616 mL
5 mM 0.4812 mL 2.4062 mL 4.8123 mL
10 mM 0.2406 mL 1.2031 mL 2.4062 mL
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In vivo Formulation Calculator (Clear solution) of CRT0066854

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 35 reference(s) in Google Scholar.)

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