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. .
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- Cell reports 34:1088992021Activity- and sleep-dependent regulation of tonic inhibition by Shisa7.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKunwei Wu,Wenyan Han,Qingjun Tian,Yan Li,Wei LuPubMed 33761345
- The Journal of biological chemistry 296:1005142021Kv1.5 channels are regulated by PKC-mediated endocytic degradation.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYuan Du,Tingzhong Wang,Jun Guo,Wentao Li,Tonghua Yang,Mark Szendrey,Shetuan ZhangPubMed 33676894
- Molecular pharmacology 96:1-122019Differential Regulation of Human Ether-à-Go-Go-Related Gene (hERG) Current and Expression by Activation of Protein Kinase C.Applications:Unspecified applicationReactive species:Unspecified reactive speciesMorgan E Sutherland-Deveen et. al.PubMed 31015282
Key facts
- CAS number
- 133052-90-1
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 412.5 Da
- Molecular formula
- C25H24N4O2
- PubChem identifier
- 2396
- Nature
- Synthetic
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
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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. .
Key facts
- CAS number
- 133052-90-1
- Purity
- > 98%
- Form
- Solid
- Molecular weight
- 412.5 Da
- Molecular formula
- C25H24N4O2
- PubChem identifier
- 2396
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 25 mM.
- Biochemical name
- Bisindolylmaleimide i
- Biological description
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.
- Canonical SMILES
- CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54
- 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)
- InChIKey
- QMGUOJYZJKLOLH-UHFFFAOYSA-N
- IUPAC name
- 3-[1-[3-(dimethylamino)propyl]indol-3-yl]-4-(1H-indol-3-yl)pyrrole-2,5-dione
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Protein Kinase C (PKC) is a family of protein kinases including isoforms such as PKC delta PKC epsilon PKC beta 2 PKC gamma PKC eta and PKC theta (also known as PRKCQ). Cyclin D1 ERK2 (Extracellular Signal-Regulated Kinase 2) GSK3 beta (Glycogen Synthase Kinase 3 beta) Cdk4 (Cyclin-Dependent Kinase 4) and PIM1 are part of this elaborate network. The mass of each protein varies for example PKC epsilon has a mass of approximately 83 kDa. These proteins express widely in different tissues but notably PRKCQ shows significant expression in T-cells while H-ERG (human Ether-à-go-go-Related Gene) primarily functions in cardiac tissues.
- 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.
- Associated diseases and disorders
PKC delta and theta relate closely to autoimmune disorders where they modulate T-cell receptor signaling contributing to immune cell activation and response. Cyclin D1 and Cdk4 have links to several cancers notably breast cancer where their dysregulation causes unchecked cellular proliferation. H-ERG is critical in disorders like long QT syndrome which affects cardiac ion channels leading to arrhythmias. GSK3 beta dysregulation is implicated in neurodegenerative diseases such as Alzheimer's disease interacting with proteins like tau exacerbating pathological conditions.
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2 product images
Chemical Structure - GF 109203X (Bisindolylmaleimide i), PKC inhibitor (ab144264)
2D chemical structure image of ab144264, GF 109203X (Bisindolylmaleimide i), PKC inhibitor
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 (Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor 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).
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