MedKoo Cat#: 531553 | Name: BIX 02565
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BIX 02565 is a novel RSK2 inhibitor with IC50 value of 1 nM. BIX 02565 inhibits adrenergic ɑ1A-, ɑ1B-, ɑ1D-, ɑ2A-, β2- and imidazoline I2 receptors with IC50 values ranging from 0.052 to 1.820 μM. These receptors played important roles in the regulation of vascular tone and cardiac function

Chemical Structure

BIX 02565
BIX 02565
CAS# 1311367-27-7

Theoretical Analysis

MedKoo Cat#: 531553

Name: BIX 02565

CAS#: 1311367-27-7

Chemical Formula: C26H30N6O2

Exact Mass: 458.2430

Molecular Weight: 458.57

Elemental Analysis: C, 68.10; H, 6.59; N, 18.33; O, 6.98

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
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Related CAS #
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Synonym
BIX 02565;BIX-02565; BIX02565.
IUPAC/Chemical Name
(5R)-N-[1-[3-(dimethylamino)propyl]benzimidazol-2-yl]-5-methyl-1-oxo-2,3,4,5-tetrahydro-[1,4]diazepino[1,2-a]indole-8-carboxamide
InChi Key
ZHMXXVNQAFCXKK-QGZVFWFLSA-N
InChi Code
InChI=1S/C26H30N6O2/c1-17-11-12-27-25(34)23-15-18-9-10-19(16-22(18)32(17)23)24(33)29-26-28-20-7-4-5-8-21(20)31(26)14-6-13-30(2)3/h4-5,7-10,15-17H,6,11-14H2,1-3H3,(H,27,34)(H,28,29,33)/t17-/m1/s1
SMILES Code
O=C(C1=CC2=C(C=C1)C=C3N2[C@H](C)CCNC3=O)NC4=NC5=CC=CC=C5N4CCCN(C)C
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
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 458.57 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Ludwik KA, Lannigan DA. Ribosomal S6 kinase (RSK) modulators: a patent review. Expert Opin Ther Pat. 2016 Sep;26(9):1061-78. doi: 10.1080/13543776.2016.1212839. PubMed PMID: 27410995. 2: Shi X, O'Neill MM, MacDonnell S, Brookes PS, Yan C, Berk BC. The RSK Inhibitor BIX02565 Limits Cardiac Ischemia/Reperfusion Injury. J Cardiovasc Pharmacol Ther. 2016 Mar;21(2):177-86. doi: 10.1177/1074248415591700. PubMed PMID: 26130615; PubMed Central PMCID: PMC4822162. 3: Edgar AJ, Trost M, Watts C, Zaru R. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2014 Feb 1;34(1). pii: e00091. PubMed PMID: 27919044; PubMed Central PMCID: PMC3908613. 4: Edgar AJ, Trost M, Watts C, Zaru R. A combination of SILAC and nucleotide acyl phosphate labelling reveals unexpected targets of the Rsk inhibitor BI-D1870. Biosci Rep. 2013 Dec 17. [Epub ahead of print] PubMed PMID: 24341623. 5: Fryer RM, Muthukumarana A, Chen RR, Smith JD, Mazurek SN, Harrington KE, Dinallo RM, Burke J, DiCapua FM, Guo X, Kirrane TM, Snow RJ, Zhang Y, Soleymanzadeh F, Madwed JB, Kashem MA, Kugler SZ, O'Neill MM, Harrison PC, Reinhart GA, Boyer SJ. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. J Pharmacol Exp Ther. 2012 Mar;340(3):492-500. doi: 10.1124/jpet.111.189365. PubMed PMID: 22128344. 6: Kirrane TM, Boyer SJ, Burke J, Guo X, Snow RJ, Soleymanzadeh L, Swinamer A, Zhang Y, Madwed JB, Kashem M, Kugler S, O'Neill MM. Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. doi: 10.1016/j.bmcl.2011.10.029. PubMed PMID: 22056746.