GF 109203X (Bisindolylmaleimide i), PKC inhibitor
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(4 Publications)
MW 412.5 Da, Purity >98%. Potent, selective PKC inhibitor (IC50 values are 0.0084, 0.0180, 0.210, 0.132, and 5.8 μM for α, β1, δ, ε and ζ isoforms respectively). Potent GSK-3 inhibitor (IC50 = 360 nM). Potent 5-HT3 antagonist (Ki = 29.5 nM). Shows anti-inflammatory effects in vivo. .
View Alternative Names
AI327039, B cell CLL/lymphoma 1, B cell leukemia 1, B-cell lymphoma 1 protein, BCL-1, BCL-1 oncogene, CCND1/FSTL3 fusion gene, CCND1/FSTL3 fusion gene, included, CCND1/IGHG1 fusion gene, CCND1/IGHG1 fusion gene, included, CCND1/IGLC1 fusion gene, CCND1/IGLC1 fusion gene, included, CCND1/PTH fusion gene, CCND1/PTH fusion gene, included, CCND1_HUMAN, CD1, CDK4 protein, CDK4_HUMAN, CMM 3, CVID9, Cell division kinase 4, Cell division protein kinase 4, Crk3, Cyclin-dependent kinase 4, Cyl 1, D11S287E, D14Ertd420e, ERK-2, ERT1, Eag-related protein 1, Ether a go go related potassium channel protein, Ether-a-go-go-related gene potassium channel 1, Ether-a-go-go-related protein 1, Extracellular signal-regulated kinase 2, G1/S-specific cyclin-D1, GSK-3 beta, GSK3B_HUMAN, GSK3beta isoform, Glycogen synthase kinase-3 beta, H-ERG, KCNH2_HUMAN, KPCA_HUMAN, KPCB_HUMAN, KPCD_HUMAN, KPCE_HUMAN, KPCG_HUMAN, KPCL_HUMAN, KPCT_HUMAN, Kinase PKC delta, Kv11.1, LQT 2, MAP kinase 1, MAP kinase 2, MAP kinase isoform p42, MAPK 1, May-01, MGC 5363, MGC125656, MGC125657, MGC126514, MGC141919, MGC14458, MGC26269, MGC49908, MGC57564, MK01_HUMAN, Melanoma cutaneous malignant 3, Mitogen-activated protein kinase 1, Mitogen-activated protein kinase 2, OTTHUMP00000043364, OTTHUMP00000043365, OTTHUMP00000067291, Oncogene PIM 1, P38, P41, PCKd, PIM, PIM1_HUMAN, PKC 0, PKC 2, PKC ZETA, PKC d, PKC delta, PKC epsilon, PKC h, PKC-A, PKC-B, PKC-L, PKC-alpha, PKC-beta, PKC-gamma, PKCC, PKCE, PKCG, PRAD1, PRAD1 oncogene, PRKC D, PRKC delta, PRKCA, PRKCB, PRKCB II, PRKCB1, PRKCB2, PRKCE, PRKCG, PRKCL, PRKCT, PRKCZ, PRKM 2, PRKM1, PSK-J3, Parathyroid adenomatosis 1, Pim 1 kinase, Pim 1 oncogene, Pkcea, Potassium channel HERG, Potassium voltage gated channel subfamily H (eag related) member 2, Potassium voltage-gated channel subfamily H member 2, Prkch, Prkcq, Protein Kinase C alpha, Protein Kinase C delta, Protein kinase C, Protein kinase C alpha type, Protein kinase C beta, Protein kinase C beta type, Protein kinase C delta VIII, Protein kinase C delta type, Protein kinase C epsilon, Protein kinase C epsilon type, Protein kinase C eta, Protein kinase C eta type, Protein kinase C gamma, Protein kinase C gamma polypeptide, Protein kinase C gamma type, Protein kinase C theta, Protein kinase C theta type, Protein kinase C zeta, Proto-oncogene serine/threonine-protein kinase Pim-1, Proviral integration site 1, Proviral integration site 2, SCA 14, SQT1, Serine/threonine-protein kinase GSK3B, Tyrosine protein kinase PRKCD, U21B31, Voltage gated potassium channel, subfamily H, member 2, Voltage-gated potassium channel subunit Kv11.1, eag homolog, hERG-1, nPKC-delta, nPKC-epsilon, nPKC-eta, nPKC-theta, p34 cdk4, p42-MAPK, pim 1 kinase 44 kDa isoform, pim 1 oncogene (proviral integration site 1), protein kinase, mitogen-activated, 1, protein kinase, mitogen-activated, 2, protein tyrosine kinase ERK2
- FuncS
Unknown
Functional Studies - GF 109203X (Bisindolylmaleimide i), PKC inhibitor (AB144264)
1.5 x 10e7 THP-1 cells were incubated with 100 nM GF 109203X (ab144264) or Ro 31-8220 mesylate (ab120374) for 30 minutes prior to activation with 10 µg x mL-1 PMA (Sigma) for 4 hours. Control cells were left without inhibitors or PMA. Cells were lysed in 1 mL of lysis buffer, and 30 µL were tested for PKC activity (duplicates; +/- SD).
- Chemical Structure
Lab
Chemical Structure - GF 109203X (Bisindolylmaleimide i), PKC inhibitor (AB144264)
2D chemical structure image of ab144264, GF 109203X (Bisindolylmaleimide i), PKC inhibitor
Properties and storage information
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Appropriate long-term storage conditions
Storage information
Supplementary information
This supplementary information is collated from multiple sources and compiled automatically.
Biological function summary
Many of these proteins regulate important cellular processes like cell cycle progression and signal transduction. Cyclin D1 acts as a regulator in the cell cycle forming a complex with Cdk4 or Cdk6 that drives transition from G1 phase to S phase. GSK3 beta is important in insulin and Wnt signaling pathways often affecting glycogen synthesis and gene transcription. PKC epsilon and PIM1 signal in cardiac and immune cells modulating cellular responses to external stimuli. H-ERG a potassium ion channel plays a substantial role in cardiac repolarization.
Pathways
PKC family members such as PKC delta and epsilon engage significantly in the NF-kB signaling pathway impacting transcriptional regulation of inflammatory cytokines. ERK2 participates in the MAPK/ERK pathway which influences cellular processes like growth differentiation and survival. Cyclin D1 and Cdk4 are essential for the transition from G1 to the S phase in the cell cycle pathway. GSK3 beta intersects with the Wnt signaling pathway altering gene expression and cellular fate. These proteins often interact with one another such as PKC isoforms which frequently modulate MAPK pathway signaling dynamics.
Publications (4)
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Molecular neurobiology 61:5129-5141 PubMed38167971
2024
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Cell reports 34:108899 PubMed33761345
2021
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The Journal of biological chemistry 296:100514 PubMed33676894
2021
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Molecular pharmacology 96:1-12 PubMed31015282
2019
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