MedKoo Biosciences

GF-109203X
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406278

CAS#: 133052-90-1

Description: GF-109203X is a potent and highly selective PCK inhibitor, which inhibits PKC isozymes alpha, beta 1, beta 2, gamma, delta and epsilon in vitro . GF-109203X inhibited GSK-3 in vitro, when assayed either in cell lysates (IC(50) 360 nM or in GSK-3beta immunoprecipitates (IC(50) 170 nM derived from rat epididymal adipocytes. Pretreatment of adipocytes with GF-109203X (5 microM) reduced GSK-3 activity in total cell lysates, to 25.1+/-4.3% of control.

Chemical Structure

GF-109203X

CAS# 133052-90-1

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 406278
Name: GF-109203X
CAS#: 133052-90-1
Chemical Formula: C25H24N4O2
Exact Mass: 412.19
Molecular Weight: 412.493
Elemental Analysis: C, 72.80; H, 5.86; N, 13.58; O, 7.76

Price and Availability

Size	Price	Availability
100mg	USD 650	2 Weeks
200mg	USD 1050	2 Weeks
500mg	USD 1850	2 Weeks
1g	USD 2950	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: GF109203X; GF-109203X; GF 109203X; bisindolylmaleimide; GO 6850; GO-6850; GO6850. BIMI.

IUPAC/Chemical Name: 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione

InChi Key: QMGUOJYZJKLOLH-UHFFFAOYSA-N

InChi Code: InChI=1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)

SMILES Code: O=C(C(C1=CN(CCCN(C)C)C2=C1C=CC=C2)=C3C4=CNC5=C4C=CC=C5)NC3=O.

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: >5 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

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Bisindolylmaleimide I (GF109203X) is a highly selective, cell-permeable, and reversible protein kinase C (PKC) inhibitor with a Ki of 14 nM.
In vitro activity:	Fig. 1B demonstrates that Bis I inhibits both short term and long term FGF2-mediated Erk activation in RCS cells. Similar data were obtained with human primary chondrocytes (Fig. 1C). Reference: J Biol Chem. 2007 Feb 2;282(5):2929-36. https://pubmed.ncbi.nlm.nih.gov/17145761/
In vivo activity:	TBD

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	3.0	7.27
	DMSO	32.3	78.37
	DMSO:PBS (pH 7.2) (1:10)	0.1	0.24
	Ethanol	1.0	2.42

Preparing Stock Solutions

The following data is based on the product molecular weight 412.493000000000000000000000000000 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.

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:	1. Krejci P, Masri B, Salazar L, Farrington-Rock C, Prats H, Thompson LM, Wilcox WR. Bisindolylmaleimide I suppresses fibroblast growth factor-mediated activation of Erk MAP kinase in chondrocytes by preventing Shp2 association with the Frs2 and Gab1 adaptor proteins. J Biol Chem. 2007 Feb 2;282(5):2929-36. doi: 10.1074/jbc.M606144200. Epub 2006 Dec 4. PMID: 17145761. 2. Hers I, Tavaré JM, Denton RM. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. doi: 10.1016/s0014-5793(99)01389-7. PMID: 10556511.
In vitro protocol:	1. Krejci P, Masri B, Salazar L, Farrington-Rock C, Prats H, Thompson LM, Wilcox WR. Bisindolylmaleimide I suppresses fibroblast growth factor-mediated activation of Erk MAP kinase in chondrocytes by preventing Shp2 association with the Frs2 and Gab1 adaptor proteins. J Biol Chem. 2007 Feb 2;282(5):2929-36. doi: 10.1074/jbc.M606144200. Epub 2006 Dec 4. PMID: 17145761. 2. Hers I, Tavaré JM, Denton RM. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. doi: 10.1016/s0014-5793(99)01389-7. PMID: 10556511.
In vivo protocol:	TBD

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1: Harmati G, Papp F, SzentandrÃ¡ssy N, BÃ¡rÃ¡ndi L, Ruzsnavszky F, HorvÃ¡th B, BÃ¡nyÃ¡sz T, Magyar J, Panyi G, Krasznai Z, NÃ¡nÃ¡si PP. Effects of the PKC inhibitors chelerythrine and bisindolylmaleimide I (GF 109203X) on delayed rectifier K+ currents. Naunyn Schmiedebergs Arch Pharmacol. 2011 Feb;383(2):141-8. doi: 10.1007/s00210-010-0584-8. Epub 2010 Dec 1. PubMed PMID: 21120453. 2: Hers I, TavarÃ© JM, Denton RM. The protein kinase C inhibitors bisindolylmaleimide I (GF 109203x) and IX (Ro 31-8220) are potent inhibitors of glycogen synthase kinase-3 activity. FEBS Lett. 1999 Nov 5;460(3):433-6. PubMed PMID: 10556511. 3: Stemmelin J, Mathis C, Ungerer A. GF 109203X, a selective inhibitor of protein kinase C, impairs retention performance in an operant task. Neuroreport. 1999 Sep 9;10(13):2805-9. PubMed PMID: 10511444. 4: Alessi DR. The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase-1beta (Rsk-2) and p70 S6 kinase. FEBS Lett. 1997 Feb 3;402(2-3):121-3. PubMed PMID: 9037179. 5: Gekeler V, Boer R, Uberall F, Ise W, Schubert C, Utz I, Hofmann J, Sanders KH, SchÃ¤chtele C, Klemm K, Grunicke H. Effects of the selective bisindolylmaleimide protein kinase C inhibitor GF 109203X on P-glycoprotein-mediated multidrug resistance. Br J Cancer. 1996 Sep;74(6):897-905. PubMed PMID: 8826855; PubMed Central PMCID: PMC2074754. 6: Grigorova-Borsos AM, Bakillah A, Urios P, Leblond V, Guillot R, Sternberg M. Production of type IV collagen and 72-kDa gelatinase by human endothelial cells cultured in high glucose. Effects of a protein kinase C inhibitor, GF 109203X. Biochem Cell Biol. 1996;74(5):659-67. PubMed PMID: 9018373. 7: Kiss Z, Phillips H, Anderson WH. The bisindolylmaleimide GF 109203X, a selective inhibitor of protein kinase C, does not inhibit the potentiating effect of phorbol ester on ethanol-induced phospholipase C-mediated hydrolysis of phosphatidylethanolamine. Biochim Biophys Acta. 1995 Feb 16;1265(1):93-5. PubMed PMID: 7857990. 8: Gekeler V, Boer R, Ise W, Sanders KH, SchÃ¤chtele C, Beck J. The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance. Biochem Biophys Res Commun. 1995 Jan 5;206(1):119-26. PubMed PMID: 7818510. 9: Le Panse R, Mitev V, Lebreton C, Coulomb B. Modulation of epidermal growth factor and keratinocyte growth factor effects on human keratinocyte growth by protein kinase C inhibitor, GF 109203X: comparison to fibroblast growth modulation. Biochem Biophys Res Commun. 1994 Nov 15;204(3):1081-7. PubMed PMID: 7980581. 10: Le Panse R, Coulomb B, Mitev V, Bouchard B, Lebreton C, Dubertret L. Differential modulation of human fibroblast and keratinocyte growth by the protein kinase C inhibitor GF 109203X. Mol Pharmacol. 1994 Sep;46(3):445-51. PubMed PMID: 7935324. 11: HeikkilÃ¤ J, Jalava A, Eriksson K. The selective protein kinase C inhibitor GF 109203X inhibits phorbol ester-induced morphological and functional differentiation of SH-SY5Y human neuroblastoma cells. Biochem Biophys Res Commun. 1993 Dec 30;197(3):1185-93. PubMed PMID: 8280132. 12: Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F, et al. The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C. J Biol Chem. 1991 Aug 25;266(24):15771-81. PubMed PMID: 1874734.

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