BIX 02565
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MedKoo CAT#: 531553

CAS#: 1311367-27-7

Description: 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

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BIX 02565
CAS# 1311367-27-7

Theoretical Analysis

MedKoo Cat#: 531553
Name: BIX 02565
CAS#: 1311367-27-7
Chemical Formula: C26H30N6O2
Exact Mass: 458.24
Molecular Weight: 458.570
Elemental Analysis: C, 68.10; H, 6.59; N, 18.33; O, 6.98

Price and Availability

Size Price Availability Quantity
5mg USD 400 2 Weeks
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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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.