GSK180736A
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MedKoo CAT#: 522708

CAS#: 817194-38-0

Description: GSK180736A is potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM25 and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).


Price and Availability

Size Price Shipping out time Quantity
50mg USD 250 2 Weeks
100mg USD 450 2 Weeks
200mg USD 750 2 Weeks
500mg USD 1650 2 Weeks
1g USD 2950 2 Weeks
2g USD 4950 2 Weeks
5g USD 6950 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-28. Prices are subject to change without notice.

GSK180736A, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522708
Name: GSK180736A
CAS#: 817194-38-0
Chemical Formula: C19H16FN5O2
Exact Mass: 365.1288
Molecular Weight: 365.3684
Elemental Analysis: C, 62.46; H, 4.41; F, 5.20; N, 19.17; O, 8.76


Synonym: GSK180736A; GSK-180736A; GSK 180736A.

IUPAC/Chemical Name: 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

InChi Key: HEAIGWIZTYAQTC-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16FN5O2/c1-10-16(17(24-19(27)22-10)11-2-4-13(20)5-3-11)18(26)23-14-6-7-15-12(8-14)9-21-25-15/h2-9,17H,1H3,(H,21,25)(H,23,26)(H2,22,24,27)

SMILES Code: CC1=C(C(NC(=O)N1)C2=CC=C(C=C2)F)C(=O)NC3=CC4=C(C=C3)NN=C4


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Waldschmidt HV, Homan KT, Cruz-Rodriguez O, Cato MC, Waninger-Saroni J,
Larimore KM, Cannavo A, Song J, Cheung JY, Kirchhoff PD, Koch WJ, Tesmer JJ,
Larsen SD. Structure-Based Design, Synthesis and Biological Evaluation of Highly
Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem.
2016 Apr 6. [Epub ahead of print] PubMed PMID: 27050625.

2: Homan KT, Waldschmidt HV, Glukhova A, Cannavo A, Song J, Cheung JY, Koch WJ,
Larsen SD, Tesmer JJ. Crystal Structure of G Protein-coupled Receptor Kinase 5 in
Complex with a Rationally Designed Inhibitor. J Biol Chem. 2015 Aug
21;290(34):20649-59. doi: 10.1074/jbc.M115.647370. Epub 2015 Jun 1. PubMed PMID:
26032411; PubMed Central PMCID: PMC4543626.

3: Homan KT, Larimore KM, Elkins JM, Szklarz M, Knapp S, Tesmer JJ.
Identification and structure-function analysis of subfamily selective G
protein-coupled receptor kinase inhibitors. ACS Chem Biol. 2015 Jan
16;10(1):310-9. doi: 10.1021/cb5006323. Epub 2014 Oct 3. PubMed PMID: 25238254;
PubMed Central PMCID: PMC4301037.