BIM-46187

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

MedKoo CAT#: 562831

CAS#: 892546-37-1

Description: 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

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BIM-46187
CAS# 892546-37-1
Instruction

Theoretical Analysis

MedKoo Cat#: 562831
Name: BIM-46187
CAS#: 892546-37-1
Chemical Formula: C44H58N8O2S2
Exact Mass: 794.41
Molecular Weight: 795.120
Elemental Analysis: C, 66.47; H, 7.35; N, 14.09; O, 4.02; S, 8.06

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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:

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.