MW 553.7 Da, Purity >98%. Widely used as a cell-permeable, reversible, competitive protein kinase C inhibitor. Also potently inhibits wide range of kinases inlcuding RSK1, RSK2, PRK2, PKCα, PKD1, MSK1, GSK3β, CDK2-cyclin A and PIM3, as well as PKCα.
Also available in simple stock solutions (ab146723) - add 1 ml of water to get an exact, ready-to-use concentration.
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Publications
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- International journal of molecular sciences 14:12873-922013A novel perspective and approach to intestinal octreotide absorption: sinomenine-mediated reversible tight junction opening and its molecular mechanism.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYuling Li,Zhijun Duan,Yan Tian,Zhen Liu,Qiuming WangPubMed 23787475
Key facts
- CAS number
- 138489-18-6
- Purity
- > 98%
- Molecular weight
- 553.7 Da
- Molecular formula
- C26H27N5O5S2
- PubChem identifier
- 11628205
- Nature
- Synthetic
Alternative names
ERK-2, ERT1, Extracellular signal-regulated kinase 2, FLJ35621, FLJ37491, HIPK1_HUMAN, Homeodomain interacting protein kinase 1 like protein, Homeodomain-interacting protein kinase 1, MAP kinase 1, MAP kinase 2, MAP kinase isoform p42, MAPK 1, MK01_HUMAN, Mitogen-activated protein kinase 1, Mitogen-activated protein kinase 2, Myak, NAD-dependent deacetylase sirtuin-2, NAD-dependent protein deacetylase sirtuin-2, Nbak 2, Nuclear body associated kinase 2, Nuclear body associated kinase 2b, P38, P41, PRKM 2, PRKM1, Regulatory protein SIR2 homolog 2, SIR2, S. cerevisiae, homolog-loke 2, SIR2-like protein 2, SIR2L, SIR2L2, SIRT 2, SIRT2_HUMAN, Silencing information regulator 2 like, Silent information regulator 2, Sir2 related protein type 2, Sirtuin (silent mating type information regulation 2 homolog) 2 (S.cerevisiae), Sirtuin 2, Sirtuin type 2, p42-MAPK, protein kinase, mitogen-activated, 1, protein kinase, mitogen-activated, 2, protein tyrosine kinase ERK2
Recommended products
MW 553.7 Da, Purity >98%. Widely used as a cell-permeable, reversible, competitive protein kinase C inhibitor. Also potently inhibits wide range of kinases inlcuding RSK1, RSK2, PRK2, PKCα, PKD1, MSK1, GSK3β, CDK2-cyclin A and PIM3, as well as PKCα.
Also available in simple stock solutions (ab146723) - add 1 ml of water to get an exact, ready-to-use concentration.
Key facts
- CAS number
- 138489-18-6
- Purity
- > 98%
- Molecular weight
- 553.7 Da
- Molecular formula
- C26H27N5O5S2
- PubChem identifier
- 11628205
- Nature
- Synthetic
- Solubility
Soluble in DMSO and organic solvents. Solubility in these solvents is approximately 20 mg/mL.
- Biochemical name
- Bisindolylmaleimide IX mesylate
- Biological description
Widely used as a cell-permeable, reversible, competitive protein kinase C inhibitor. Also potently inhibits wide range of kinases inlcuding RSK1, RSK2, PRK2, PKCα, PKD1, MSK1, GSK3β, CDK2-cyclin A and PIM3, as well as PKCα.
Also available in simple stock solutions (ab146723) - add 1 ml of water to get an exact, ready-to-use concentration.- Canonical SMILES
- CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)CCCSC(=N)N.CS(=O)(=O)O
- InChI
- InChI=1S/C25H23N5O2S.CH4O3S/c1-29-13-17(15-7-2-4-9-19(15)29)21-22(24(32)28-23(21)31)18-14-30(11-6-12-33-25(26)27)20-10-5-3-8-16(18)20;1-5(2,3)4/h2-5,7-10,13-14H,6,11-12H2,1H3,(H3,26,27)(H,28,31,32);1H3,(H,2,3,4)
- InChIKey
- SAWVGDJBSPLRRB-UHFFFAOYSA-N
- IUPAC name
- methanesulfonic acid;3-[3-[4-(1-methylindol-3-yl)-2,5-dioxopyrrol-3-yl]indol-1-yl]propyl carbamimidothioate
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
ERK2 also known as extracellular signal-regulated kinase 2 is a protein that plays a role in the MAP kinase signaling pathway which is important for various cellular processes. It has a mass of approximately 42 kDa. ERK2 expression occurs across many tissues with high levels in the brain heart and skeletal muscle. SIRT2 or sirtuin 2 is an NAD+-dependent deacetylase involved in metabolic regulation and has a mass of about 43 kDa. It is found in the cytoplasm and nuclear compartments in several cell types. HIPK1 or homeodomain-interacting protein kinase 1 functions as a serine/threonine kinase and its mass is about 133 kDa. It is expressed in the nucleus in tissues including the brain and kidney.
- Biological function summary
ERK2 SIRT2 and HIPK1 participate in significant cellular regulation. ERK2 acts in signal transduction to regulate cell division and differentiation. SIRT2 deacetylates proteins contributing to the regulation of glucose homeostasis and stress responses. HIPK1 interacts with transcription factors modulating gene expression in response to cellular stress. These proteins might participate in larger complexes that influence cellular responses tissues development and homeostasis.
- Pathways
ERK2 is an important component of the MAPK/ERK pathway involved in transmitting signals from the cell surface to the DNA influencing growth and survival. SIRT2 participates in the regulation of the insulin signaling pathway affecting metabolic processes. Both proteins intersect through their modulation of cell cycle progression and apoptotic pathways. HIPK1 plays roles in the Wnt signaling pathway linking to transcriptional regulation and cell fate determination and it also interacts with proteins in these pathways to influence cell survival and differentiation.
- Associated diseases and disorders
ERK2 SIRT2 and HIPK1 serve as contributors to different pathological conditions. Hyperactivity of ERK2 correlates with cancer progression due to its impact on cell proliferation. SIRT2 involvement connects to neurodegenerative diseases like Parkinson’s through its regulation of cellular stress responses. HIPK1's dysregulation may link to cancer development as well. These proteins often engage with others like protein kinase A (PKA) in cancer or alpha-synuclein in neurodegenerative disorders influencing disease outcomes and progression.
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2 product images
Chemical Structure - Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor (ab120374)
2D chemical structure image of ab120374, Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor
Functional Studies - Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor (ab120374)
1.5 x 10e7 THP-1 cells were incubated with 100 nM GF 109203X (GF 109203X (Bisindolylmaleimide i), PKC inhibitor 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).
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