MedKoo Cat#: 562831 | Name: BIM-46187
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Description:

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

BIM-46187 is a pan G protein inhibitor. It specifically silences Gαq proteins by "freezing" Gαq in its empty pocket conformation, a conformational intermediate along the Gα activation pathway.

Chemical Structure

BIM-46187
BIM-46187
CAS#892546-37-1

Theoretical Analysis

MedKoo Cat#: 562831

Name: BIM-46187

CAS#: 892546-37-1

Chemical Formula: C44H58N8O2S2

Exact Mass: 794.4124

Molecular Weight: 795.12

Elemental Analysis: C, 66.47; H, 7.35; N, 14.09; O, 4.02; S, 8.06

Price and Availability

Size Price Availability Quantity
25mg USD 750.00 2 Weeks
50mg USD 1,250.00 2 Weeks
100mg USD 2,050.00 2 Weeks
1g USD 5,950.00 2 Weeks
2g USD 8,650.00 2 Weeks
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Related CAS #
No Data
Synonym
BIM-46187; BIM 46187; BIM46187; PH-064; PH 064; PH064;
IUPAC/Chemical Name
(2R,2'R)-3,3'-disulfanediylbis(2-amino-1-((S)-8-(cyclohexylmethyl)-2-phenyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)propan-1-one)
InChi Key
GGDNOAWICIHSAW-KEAHXZLPSA-N
InChi Code
InChI=1S/C44H58N8O2S2/c45-35(43(53)51-23-21-49-27-37(33-17-9-3-10-18-33)47-41(49)39(51)25-31-13-5-1-6-14-31)29-55-56-30-36(46)44(54)52-24-22-50-28-38(34-19-11-4-12-20-34)48-42(50)40(52)26-32-15-7-2-8-16-32/h3-4,9-12,17-20,27-28,31-32,35-36,39-40H,1-2,5-8,13-16,21-26,29-30,45-46H2/t35-,36-,39-,40-/m0/s1
SMILES Code
O=C([C@@H](N)CSSC[C@H](N)C(N1[C@@H](CC2CCCCC2)C3=NC(C4=CC=CC=C4)=CN3CC1)=O)N5[C@@H](CC6CCCCC6)C7=NC(C8=CC=CC=C8)=CN7CC5
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 795.12 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: Kanarek AM, Wagner A, Küppers J, Gütschow M, Postina R, Kojro E. Crosstalk between angiotensin and the nonamyloidogenic pathway of Alzheimer's amyloid precursor protein. FEBS J. 2017 Mar;284(5):742-753. doi: 10.1111/febs.14015. Epub 2017 Feb 10. PubMed PMID: 28102934. 2: Schmitz AL, Schrage R, Gaffal E, Charpentier TH, Wiest J, Hiltensperger G, Morschel J, Hennen S, Häußler D, Horn V, Wenzel D, Grundmann M, Büllesbach KM, Schröder R, Brewitz HH, Schmidt J, Gomeza J, Galés C, Fleischmann BK, Tüting T, Imhof D, Tietze D, Gütschow M, Holzgrabe U, Sondek J, Harden TK, Mohr K, Kostenis E. A cell-permeable inhibitor to trap Gαq proteins in the empty pocket conformation. Chem Biol. 2014 Jul 17;21(7):890-902. doi: 10.1016/j.chembiol.2014.06.003. PubMed PMID: 25036778; PubMed Central PMCID: PMC4337399. 3: Ouelaa-Benslama R, De Wever O, Hendrix A, Sabbah M, Lambein K, Land D, Prévost G, Bracke M, Hung MC, Larsen AK, Emami S, Gespach C. Identification of a GαGβγ, AKT and PKCα signalome associated with invasive growth in two genetic models of human breast cancer cell epithelial-to-mesenchymal transition. Int J Oncol. 2012 Jul;41(1):189-200. doi: 10.3892/ijo.2012.1457. Epub 2012 Apr 30. PubMed PMID: 22552300. 4: Dessein AF, Stechly L, Jonckheere N, Dumont P, Monté D, Leteurtre E, Truant S, Pruvot FR, Figeac M, Hebbar M, Lecellier CH, Lesuffleur T, Dessein R, Grard G, Dejonghe MJ, de Launoit Y, Furuichi Y, Prévost G, Porchet N, Gespach C, Huet G. Autocrine induction of invasive and metastatic phenotypes by the MIF-CXCR4 axis in drug-resistant human colon cancer cells. Cancer Res. 2010 Jun 1;70(11):4644-54. doi: 10.1158/0008-5472.CAN-09-3828. Epub 2010 May 11. PubMed PMID: 20460542. 5: Ayoub MA, Damian M, Gespach C, Ferrandis E, Lavergne O, De Wever O, Banères JL, Pin JP, Prévost GP. Inhibition of heterotrimeric G protein signaling by a small molecule acting on Galpha subunit. J Biol Chem. 2009 Oct 16;284(42):29136-45. doi: 10.1074/jbc.M109.042333. Epub 2009 Jul 31. PubMed PMID: 19648112; PubMed Central PMCID: PMC2781458. 6: Favre-Guilmard C, Zeroual-Hider H, Soulard C, Touvay C, Chabrier PE, Prevost G, Auguet M. The novel inhibitor of the heterotrimeric G-protein complex, BIM-46187, elicits anti-hyperalgesic properties and synergizes with morphine. Eur J Pharmacol. 2008 Oct 10;594(1-3):70-6. doi: 10.1016/j.ejphar.2008.07.016. Epub 2008 Jul 15. PubMed PMID: 18664366.