GSK1210151A (I-BET151)
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MedKoo CAT#: 406154

CAS#: 1300031-49-5

Description: GSK1210151A, also known as I-BET151, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 ( GSK1210151A ) shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.


Chemical Structure

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GSK1210151A (I-BET151)
CAS# 1300031-49-5

Theoretical Analysis

MedKoo Cat#: 406154
Name: GSK1210151A (I-BET151)
CAS#: 1300031-49-5
Chemical Formula: C23H21N5O3
Exact Mass: 415.16444
Molecular Weight: 415.44
Elemental Analysis: C, 66.49; H, 5.09; N, 16.86; O, 11.55

Price and Availability

Size Price Availability Quantity
25.0mg USD 250.0 2 Weeks
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
200.0mg USD 1250.0 2 Weeks
500.0mg USD 1950.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 5250.0 2 Weeks
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Synonym: IBET151; IBET-151; IBET 151; GSK1210151A; GSK-1210151A; GSK 1210151A.

IUPAC/Chemical Name: 7-(3,5-dimethylisoxazol-4-yl)-8-methoxy-1-((R)-1-(pyridin-2-yl)ethyl)-1H-imidazo[4,5-c]quinolin-2(3H)-one

InChi Key: VUVUVNZRUGEAHB-CYBMUJFWSA-N

InChi Code: InChI=1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1

SMILES Code: O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3

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

Preparing Stock Solutions

The following data is based on the product molecular weight 415.44 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

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1: Halper-Stromberg A, Lu CL, Klein F, Horwitz JA, Bournazos S, Nogueira L, Eisenreich TR, Liu C, Gazumyan A, Schaefer U, Furze RC, Seaman MS, Prinjha R, Tarakhovsky A, Ravetch JV, Nussenzweig MC. Broadly neutralizing antibodies and viral inducers decrease rebound from HIV-1 latent reservoirs in humanized mice. Cell. 2014 Aug 28;158(5):989-99. doi: 10.1016/j.cell.2014.07.043. Epub 2014 Aug 14. PubMed PMID: 25131989; PubMed Central PMCID: PMC4163911.

2: Barrett E, Brothers S, Wahlestedt C, Beurel E. I-BET151 selectively regulates IL-6 production. Biochim Biophys Acta. 2014 Sep;1842(9):1549-55. doi: 10.1016/j.bbadis.2014.05.013. Epub 2014 May 22. PubMed PMID: 24859008; PubMed Central PMCID: PMC4125491.

3: Pastori C, Daniel M, Penas C, Volmar CH, Johnstone AL, Brothers SP, Graham RM, Allen B, Sarkaria JN, Komotar RJ, Wahlestedt C, Ayad NG. BET bromodomain proteins are required for glioblastoma cell proliferation. Epigenetics. 2014 Apr;9(4):611-20. doi: 10.4161/epi.27906. Epub 2014 Feb 19. PubMed PMID: 24496381; PubMed Central PMCID: PMC4121371.

4: Chaidos A, Caputo V, Gouvedenou K, Liu B, Marigo I, Chaudhry MS, Rotolo A, Tough DF, Smithers NN, Bassil AK, Chapman TD, Harker NR, Barbash O, Tummino P, Al-Mahdi N, Haynes AC, Cutler L, Le B, Rahemtulla A, Roberts I, Kleijnen M, Witherington JJ, Parr NJ, Prinjha RK, Karadimitris A. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705. doi: 10.1182/blood-2013-01-478420. Epub 2013 Dec 13. PubMed PMID: 24335499.

5: Alsarraj J, Faraji F, Geiger TR, Mattaini KR, Williams M, Wu J, Ha NH, Merlino T, Walker RC, Bosley AD, Xiao Z, Andresson T, Esposito D, Smithers N, Lugo D, Prinjha R, Day A, Crawford NP, Ozato K, Gardner K, Hunter KW. BRD4 short isoform interacts with RRP1B, SIPA1 and components of the LINC complex at the inner face of the nuclear membrane. PLoS One. 2013 Nov 19;8(11):e80746. doi: 10.1371/journal.pone.0080746. eCollection 2013. PubMed PMID: 24260471; PubMed Central PMCID: PMC3834312.

6: Tolani B, Gopalakrishnan R, Punj V, Matta H, Chaudhary PM. Targeting Myc in KSHV-associated primary effusion lymphoma with BET bromodomain inhibitors. Oncogene. 2014 May 29;33(22):2928-37. doi: 10.1038/onc.2013.242. Epub 2013 Jun 24. PubMed PMID: 23792448.

7: Boehm D, Calvanese V, Dar RD, Xing S, Schroeder S, Martins L, Aull K, Li PC, Planelles V, Bradner JE, Zhou MM, Siliciano RF, Weinberger L, Verdin E, Ott M. BET bromodomain-targeting compounds reactivate HIV from latency via a Tat-independent mechanism. Cell Cycle. 2013 Feb 1;12(3):452-62. doi: 10.4161/cc.23309. Epub 2012 Feb 1. PubMed PMID: 23255218; PubMed Central PMCID: PMC3587446.

8: Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK. Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A). Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24. PubMed PMID: 22437115.

9: Mirguet O, Lamotte Y, Donche F, Toum J, Gellibert F, Bouillot A, Gosmini R, Nguyen VL, Delannée D, Seal J, Blandel F, Boullay AB, Boursier E, Martin S, Brusq JM, Krysa G, Riou A, Tellier R, Costaz A, Huet P, Dudit Y, Trottet L, Kirilovsky J, Nicodeme E. From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125. Epub 2012 Feb 8. PubMed PMID: 22386529.

10: Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T. Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia. Nature. 2011 Oct 2;478(7370):529-33. doi: 10.1038/nature10509. PubMed PMID: 21964340; PubMed Central PMCID: PMC3679520.



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