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AB144402

SB 505124, ALK5 inhibitor

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(2 Publications)

MW 335.4 Da, Purity >98%. Potent, reversible, competitive ALK5 inhibitor (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). Inhibits ALK7 but not ALK1, 2, 3, or 6. Shows antifibrotic effects in vivo. .

View Alternative Names

AAT 5, ACTR-IB, ACV1B_HUMAN, ACVR 1B, ACVRLK 4, ALK-4, ALK-5, Activin A receptor type 1B, Activin A receptor type II like kinase, Activin A receptor type II like kinase 4, Activin A receptor type II like kinase 53kDa, Activin A receptor type II like kinase, 53kD, Activin A type 1B receptor, Activin A type IB receptor, Activin receptor type IB, Activin receptor type-1B, Activin receptor-like kinase 4, Activin receptor-like kinase 5, CARD 3, CARD carrying kinase, CARD containing ICE associated kinase, CARD containing interleukin 1 beta converting enzyme (ICE) associated kinase, CARD-containing IL-1 beta ICE-kinase, CARD-containing interleukin-1 beta-converting enzyme-associated kinase, CARDIAK, CLARP kinase, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSPB1, Csaids binding protein, Cytokine suppressive anti-inflammatory drug-binding protein, EXIP, GIG 30, Growth inhibiting gene 30, IMD42, LDS1A, LDS2A, MAP kinase 14, MAP kinase MXI2, MAP kinase p38 alpha, MAPK 14, MAX-interacting protein 2, MGC129539, MK14_HUMAN, MSSE, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Mxi 2, NR1F3, Nuclear receptor ROR-gamma, Nuclear receptor RZR-gamma, Nuclear receptor subfamily 1 group F member 3, P38, PRKM14, PRKM15, RAR related orphan nuclear receptor variant 2, RAR related orphan receptor C, isoform a, RAR related orphan receptor gamma, RAR-related orphan receptor C, RICK, RIP-like-interacting CLARP kinase, RIPK2_HUMAN, RK, RORG_HUMAN, RZR GAMMA, RZRG, Receptor interacting protein (RIP) like interacting caspase like apoptosis regulatory protein (CLARP) kinase, Receptor interacting serine threonine kinase 2, Receptor-interacting protein 2, Receptor-interacting serine/threonine-protein kinase 2, Retinoic acid binding receptor gamma, Retinoid-related orphan receptor-gamma, Rorc, SAPK2A, SKR 2, SKR 4, Serine(threonine) protein kinase receptor R2, Serine/threonine-protein kinase receptor R2, Serine/threonine-protein kinase receptor R4, Stress-activated protein kinase 2a, TGF-beta receptor type I, TGF-beta receptor type-1, TGF-beta type I receptor, TGFBR 1, TGFBR1 protein, TGFR1_HUMAN, TNFRSF, TOR, TbetaR-I, Transforming growth factor beta receptor 1, Transforming growth factor beta receptor I, Transforming growth factor beta receptor I (activin A receptor type II like kinase, 53kD), Transforming growth factor-beta receptor type I, Tyrosine-protein kinase RIPK2, UNQ277/PRO314/PRO34092, activin A receptor type II-like protein kinase of 53kD, p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip

Key facts

CAS number

356559-13-2

Purity

>98%

Form

Solid

form

Molecular weight

335.4 Da

Molecular formula

C<sub>2</sub><sub>0</sub>H<sub>2</sub><sub>1</sub>N<sub>3</sub>O<sub>2</sub>

PubChem

9858940

Nature

Synthetic

Solubility

Soluble in ethanol to 100 mM

Soluble in DMSO to 100 mM

Biochemical name

2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine

Biological description

Potent, reversible, competitive ALK5 inhibitor (IC50 values are 47 and 129 nM for ALK5 and ALK4 respectively). Inhibits ALK7 but not ALK1, 2, 3, or 6. Shows antifibrotic effects in vivo.

Canonical smiles

CC1=NC(=CC=C1)C2=C(N=C(N2)C(C)(C)C)C3=CC4=C(C=C3)OCO4

InChi

InChI=1S/C20H21N3O2/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15/h5-10H,11H2,1-4H3,(H,22,23)

InChiKey

WGZOTBUYUFBEPZ-UHFFFAOYSA-N

IUPAC Name

2-[4-(1,3-benzodioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl]-6-methylpyridine

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

Supplementary information

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

The p38 kinase also known as MAPK14 weighs about 41 kDa. It is expressed in many tissues such as the heart brain skeletal muscle and liver. Mechanically it acts as a serine/threonine kinase part of the mitogen-activated protein kinase (MAPK) family. RIP2 or receptor-interacting serine/threonine-protein kinase 2 is associated with receptor complexes in immune responses. TGF beta Receptor I also known as ALK-5 is a part of the TGF-beta receptor complex and is widely expressed in various tissues. Activin A Receptor Type IB or ALK-4 has a mass of 56 kDa and shows expression in the ovary muscle and brain. ROR gamma or retinoic acid receptor-related orphan receptor gamma is expressed largely in lymphoid tissues especially in the thymus.
Biological function summary

P38 kinase functions include the transmission of signals for inflammation cell differentiation and apoptosis. It often functions as part of larger pathways like the MAPK cascade. RIP2 participates in innate immune responses functioning within the NOD1/2 signaling complex. TGF beta Receptor I mediates the TGF-beta signaling pathways that regulate cell growth and differentiation often associating with type II receptors to form heterodimers. Activin A Receptor Type IB can form a complex with type II receptors to modulate reproductive and developmental processes. ROR gamma plays an important role in the development of immune cell lineages and circadian rhythm regulation.

Pathways

P38 kinase plays a significant role in the MAPK signaling pathway and is linked with proteins like JNK and ERK which are also part of MAPK family. RIP2 is pivotal in the NOD-like receptor signaling pathway engaging proteins like CARD9 for facilitating immune responses. TGF beta Receptor I being integral to the TGF-beta signaling pathway interacts heavily with SMAD proteins. Activin A Receptor Type IB fits into the Activin signaling pathway which involves different SMAD proteins. ROR gamma is involved in the nuclear receptor signaling pathway interacting with proteins such as ROR alpha and dermokine for metabolic and developmental regulation.

The p38 kinase association includes inflammatory diseases and cancer engaging with proteins like NF-kB that mediate inflammation. Alterations in RIP2 can lead to inflammatory disorders such as Crohn's disease with connections to inflammatory cytokines. TGF beta Receptor I frequently links to fibrosis and cancer as it engages pathways involving SMAD3. Mutations or dysregulation of Activin A Receptor Type IB often relate to reproductive disorders and cancers interacting with proteins such as Follistatin. ROR gamma is involved in autoimmune diseases such as psoriasis affecting the function of IL-17-producing immune cells.

Product protocols

Publications (2)

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

Cell cycle (Georgetown, Tex.) 16:879-893 PubMed28426320

2017

Transient exposure to androgens induces a remarkable self-sustained quiescent state in dispersed prostate cancer cells.

Applications

Unspecified application

Species

Unspecified reactive species

Anh Thu Bui,Meng-Er Huang,Maryline Havard,Fanny Laurent-Tchenio,François Dautry,Thierry Tchenio

Cell cycle (Georgetown, Tex.) 14:1218-31 PubMed25706341

2015

SMAD signaling and redox imbalance cooperate to induce prostate cancer cell dormancy.

Applications

Unspecified application

Species

Unspecified reactive species

Anh Thu Bui,Fanny Laurent,Maryline Havard,François Dautry,Thierry Tchénio
View all publications

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