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
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Supplementary information
This supplementary information is collated from multiple sources and compiled automatically.
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.
Publications (2)
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Cell cycle (Georgetown, Tex.) 16:879-893 PubMed28426320
2017
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Cell cycle (Georgetown, Tex.) 14:1218-31 PubMed25706341
2015
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