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GF109203X - ≥99%, high purity , CAS No.133052-90-1, Inhibitor of protein kinase C alpha;Inhibitor of protein kinase C beta;Inhibitor of protein kinase C gamma

Specifications & Purity: ≥99%

CAS#: 133052-90-1
Formula: C₂₅H₂₄N₄O₂
Molecular Weight: 412.48
MDL number: MFCD00236428
PubChem CID: 2396

Item Number

G129390

Grouped product items
SKU	Size	Availability	Price
G129390-1mg	1mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$18.90
G129390-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$75.90
G129390-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$129.90
G129390-50mg	50mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$489.90

Potent, selective PKC inhibitor. Potent GSK-3 inhibitor. Potent 5-HT3 antagonist.

View related series

protein kinase C alpha Inhibitor protein kinase C beta Inhibitor protein kinase C gamma Inhibitor

Basic Description

Synonyms	bisindolylmaleimide i\|133052-90-1\|GF 109203X\|GF109203X\|GF-109203X\|Go 6850\|Go-6850\|3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione\|3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione\|Bisindolylm
Specifications & Purity	≥99%
Storage Temp	Store at 2-8°C
Shipped In	Wet ice
Action Type	INHIBITOR
Mechanism of action	Inhibitor of protein kinase C alpha;Inhibitor of protein kinase C beta;Inhibitor of protein kinase C gamma

Associated Targets

PIM1 Tchem Serine/threonine-protein kinase pim-1 3 Activities

Discover Target: PIM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCD Tclin Protein kinase C delta type 1 Activities

Discover Target: PRKCD

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCB Tchem Protein kinase C beta type 1 Activities

Discover Target: PRKCB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCE Tchem Protein kinase C epsilon type 3 Activities

Discover Target: PRKCE

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCH Tchem Protein kinase C eta type 1 Activities

Discover Target: PRKCH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LMTK3 Tchem Serine/threonine-protein kinase LMTK3 2 Activities

Discover Target: LMTK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 1 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCG Tchem Protein kinase C gamma type 0 Activities

Discover Target: PRKCG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCA Tchem Protein kinase C alpha type 2 Activities

Discover Target: PRKCA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PRKCQ Tchem Protein kinase C theta type 1 Activities

Discover Target: PRKCQ

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
INCHI	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)
InChi Key	QMGUOJYZJKLOLH-UHFFFAOYSA-N
Canonical SMILES	CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
Isomeric SMILES	CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
WGK Germany	3
RTECS	UX9590000
PubChem CID	2396
Molecular Weight	412.48

CAS Registry No.

PubChem CID

ChEMBL Ligand

Wikipedia

RCSB PDB Ligand

Certificates

Certificate of Analysis(COA)

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3 results found

Lot Number	Certificate Type	Date	Item
H1520114	Certificate of Analysis	Apr 12, 2023	G129390
K2306144	Certificate of Analysis	Apr 12, 2023	G129390
K2306146	Certificate of Analysis	Apr 12, 2023	G129390

Solubility

Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.

Sensitivity

Heat Sensitive

Melt Point(°C)

270 °C

Pictogram(s)

GHS07

Signal

Warning

Hazard Statements

H302

Precautionary Statements

P501,P264,P270,P330,P301+P317

WGK Germany

RTECS

UX9590000

References

1. Toullec D, Pianetti P, Coste H, Bellevergue P, Grand-Perret T, Ajakane M, Baudet V, Boissin P, Boursier E, Loriolle F et al.. (1991) The bisindolylmaleimide GF 109203X is a potent and selective inhibitor of protein kinase C.. J Biol Chem, 266 (24): (15771-81). [PMID:1874734]
2. Wu K et al.. (2021) Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.. Cell Rep, 34 (12): (108899). [PMID:33761345]
3. Sutherland-Deveen ME et al.. (2019) Differential Regulation of Human Ether-à-Go-Go-Related Gene (hERG) Current and Expression by Activation of Protein Kinase C.. Mol Pharmacol, 96 (1-12). [PMID:31015282]
4. Du Y et al.. (2021) Kv1.5 channels are regulated by PKC-mediated endocytic degradation.. J Biol Chem, 296 (100514). [PMID:33676894]

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