ALK5
ALK5, also known as transforming growth factor-β type I receptor (TGFβRI/TβRI), is a serine/threonine kinase receptor that functions as a central mediator of canonical TGF-β signaling and transduces extracellular TGF-β cues into intracellular transcriptional responses through receptor-regulated signaling cascades[1][2]. Mechanistically, ALK5 forms a receptor complex with TGF-β type II receptor and mediates downstream signaling through phosphorylation-dependent pathways, including activation of Smad proteins that regulate gene expression and cellular responses[1][3]. Through these signaling mechanisms, ALK5 contributes to biological processes associated with extracellular matrix production, cellular proliferation, migration, and morphologic regulation, making it a widely used target in studies of fibrosis and cancer-related signaling[1][4]. In disease and experimental models, pharmacological inhibition of ALK5 suppresses TGF-β-induced extracellular matrix production, inhibits TGF-β-mediated cellular responses, and reduces proliferation or motility in multiple cell systems[1][4]. Compared with related activin receptor-like kinases, ALK5 belongs to the TGF-β signaling branch and is closely related to ALK4 and ALK7, whereas BMP-responsive receptors such as ALK1, ALK2, ALK3, and ALK6 exhibit distinct signaling specificities[3]. For experimental applications, the small-molecule inhibitor SB-431542 is one of the most extensively characterized ALK5 inhibitors and selectively targets ALK5 together with ALK4 and ALK7 while sparing BMP receptor signaling and several MAP kinase pathways, providing a valuable tool for dissecting TGF-β-dependent biological mechanisms[3].
References:
- [1]. Ungefroren H, et al. Signaling Crosstalk of TGF-β/ALK5 and PAR2/PAR1: A Complex Regulatory Network Controlling Fibrosis and Cancer. Int J Mol Sci. 2018 May 24;19(6):1568. [Content Brief]
- [2]. Wikipedia.
- [3]. Inman GJ, et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2002 Jul;62(1):65-74. [Content Brief]
- [4]. Ali SR, et al. Nerve Density and Neuronal Biomarkers in Cancer. Cancers (Basel). 2022 Oct 1;14(19):4817. [Content Brief]
All Product Categories
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ALK5 Related Products (31)
Related Products (31)
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Recombinant Proteins (7)
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CDD-2789
0 ImagesCat. No.: HY-173149CAS No.: 3052084-77-9
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M4K2281
0 ImagesCat. No.: HY-161376CAS No.: 3034840-19-9M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h.
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ALK5-IN-33
0 ImagesCat. No.: HY-151283CAS No.: 2785430-89-7ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC50 ≤10 nM.
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J-1149
0 ImagesCat. No.: HY-163429CAS No.: 2883580-95-6
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Finbosertib
0 ImagesCat. No.: HY-178231CAS No.: 2766583-86-0Synonyms: ALK5-IN-85
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ALK5-IN-25
0 ImagesCat. No.: HY-151270CAS No.: 2785430-81-9ALK5-IN-25 (compound EX-02) is a potent ALK-5 inhibitor with an IC50 ≤10 nM.ALK5-IN-25 also inhibits ALK-2 (selectivity ALK2/ALK5≤10). ALK5-IN-25 can be used for the research of cancer.
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ALK5-IN-27
0 ImagesCat. No.: HY-151273CAS No.: 2785430-83-1ALK5-IN-27 (Compound EX-04) is a potent ALK-5 inhibitor with an IC50 ≤10 nM. ALK5-IN-27 also inhibits ALK-2 (selectivity ALK2/ALK5 ≤10).
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J-1063
0 ImagesCat. No.: HY-145855CAS No.: 2374772-46-8
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ALK5-IN-28
0 ImagesCat. No.: HY-151275CAS No.: 2785430-84-2ALK5-IN-28 (Compound Ex-05) is a selective ALK-5 inhibitor (IC50 ≤ 10 nM) that inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit tumor growth in vivo. ALK5-IN-28 can be used in the research of proliferative diseases such as cancer.
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M4K2306
0 ImagesCat. No.: HY-161377CAS No.: 3034840-25-7M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6.
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