JavaScript is disabled in your browser. Please enable JavaScript to view this website.
AB120374

Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor

Be the first to review this product! Submit a review

|

(1 Publication)

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.

View 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

2 Images
Functional Studies - Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor (AB120374)
  • FuncS

Unknown

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 (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 - Ro 31-8220 mesylate (Bisindolylmaleimide IX), Protein kinase inhibitor (AB120374)
  • Chemical Structure

Lab

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

Key facts

CAS number

138489-18-6

Purity

>98%

Molecular weight

553.7 Da

Molecular formula

C<sub>2</sub><sub>6</sub>H<sub>2</sub><sub>7</sub>N<sub>5</sub>O<sub>5</sub>S<sub>2</sub>

PubChem

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

style
left-column
style
left-column
style
left-column

Properties and storage information

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
style
left-column

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

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.

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.
style
left-column

Product protocols

For this product, it's our understanding that no specific protocols are required. You can visit:
style
left-column

Publications (1)

Recent publications for all applications. Explore the full list and refine your search

International journal of molecular sciences 14:12873-92 PubMed23787475

2013

A novel perspective and approach to intestinal octreotide absorption: sinomenine-mediated reversible tight junction opening and its molecular mechanism.

Applications

Unspecified application

Species

Unspecified reactive species

Yuling Li,Zhijun Duan,Yan Tian,Zhen Liu,Qiuming Wang
View all publications
style
left-column
style
left-column

Product promise

We are committed to supporting your work with high-quality reagents, and we're here for you every step of the way. In the unlikely event that one of our products does not perform as expected, you're protected by our Product Promise.
For full details, please see our Terms & Conditions
style
left-column
style
right-column
style
bg-slate-100

Please note: All products are 'FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR THERAPEUTIC PROCEDURES'.

For licensing inquiries, please contact partnerships@abcam.com