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ALK5 inhibitor

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61

Inhibitors & Agonists

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Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-144043
    ALK5-IN-8

    		TGF-β Receptor Cancer
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1) .
    ALK5-IN-8
  • HY-151289
    ALK5-IN-34

    		TGF-β Receptor TGF-beta/Smad Cancer
    ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC50 value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
    ALK5-IN-34
  • HY-161662
    ALK5-IN-80

    		TGF-β Receptor Cancer
    ALK5-IN-80 (Compound 29b) is a selective ALK5 inhibitor with an IC50 value of 3.7 nM. ALK5-IN-80 can be used for cancer research .
    ALK5-IN-80
  • HY-163507
    ALK5-IN-79

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
    ALK5-IN-79
  • HY-159952
    ALK5-IN-84

    		Anaplastic lymphoma kinase (ALK) Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    ALK5-IN-84 (Compound 23) is an ALK5 inhibitor with a pKi value of 9.35 against hALK5. When administered via inhalation, ALK5-IN-84 exhibits significant ALK5 inhibitory activity. ALK5-IN-84 is promising for the development of inhaled ALK5 inhibitors .
    ALK5-IN-84
  • HY-151273
    ALK5-IN-27

    		TGF-β Receptor Cancer
    ALK5-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) .
    ALK5-IN-27
  • HY-151272
    ALK5-IN-26

    		Others Cancer
    ALK5-IN-26 (EX-22) is an ALK (Activin receptor-like kinase) inhibitor. ALK5-IN-26 inhibits ALK5 with an IC50 value ≤10 nM. ALK5-IN-26 can be used for the research of cancer .
    ALK5-IN-26
  • HY-151270
    ALK5-IN-25

    		TGF-β Receptor Cancer
    ALK5-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 .
    ALK5-IN-25
  • HY-144437
    ALK5-IN-9

    		TGF-β Receptor Cancer
    ALK5-IN-9 (Compound 8h) is a potent and orally active inhibitor of TGFβRI (ALK5). ALK5-IN-9 inhibits ALK5 autophosphorylation and NIH3T3 cell activity with IC50 values of 25 nM and 74.6 nM, respectively. ALK5-IN-9 also shows favorable pharmacokinetic profile and ameliorated hERG inhibition. ALK5-IN-9 has the potential for the research of cancer disease .
    ALK5-IN-9
  • HY-151277
    ALK5-IN-29

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-29 is an selective activin receptor-like kinase (ALK) inhibitor. ALK5-IN-29 can inhibit the activity of ALK5 with an IC50 value of ≤10 nM. ALK5-IN-29 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer .
    ALK5-IN-29
  • HY-151275
    ALK5-IN-28

    		TGF-β Receptor TGF-beta/Smad Cancer
    ALK5-IN-28 (compound Ex-05) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-28 has the potential to inhibit growth of tumour in vivo. ALK5-IN-28 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis .
    ALK5-IN-28
  • HY-151281
    ALK5-IN-31

    		TGF-β Receptor Cancer
    ALK5-IN-31 (compound Ex-08) is a selective ALK-5 inhibitor (IC50≤10 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-31 has the potential to inhibit growth of tumour in vivo. ALK5-IN-31 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis .
    ALK5-IN-31
  • HY-151233
    ALK5-IN-10

    		TGF-β Receptor Cancer
    ALK5-IN-10 (Compound 5d) is a TGF-β type I receptor kinase ALK5 inhibitor, with IC50s of 0.007 and 1.98 μM for ALK5 and p38α, respectively. ALK5-IN-10 can be used for the research of cancer .
    ALK5-IN-10
  • HY-151282
    ALK5-IN-32

    		TGF-β Receptor TGF-beta/Smad Cancer
    ALK5-IN-32 (compound EX-09) is a selective ALK-5 inhibitor (10 nM<IC50<100 nM), inhibits TGF-β-induced SMAD signaling. ALK5-IN-32 has the potential to inhibit growth of tumour in vivo. ALK5-IN-32 can be used in study of proliferative diseases such as cancer, fibrotic diseases, and systemic sclerosis .
    ALK5-IN-32
  • HY-151283
    ALK5-IN-33

    		TGF-β Receptor Cancer
    ALK5-IN-33 (Compound EX-10) is a selective, orally active ALK-5 inhibitor with an IC50 ≤10 nM .
    ALK5-IN-33
  • HY-168607
    ALK5-IN-83

    		TGF-beta/Smad Cancer
    ALK5-IN-83 (compound 13b) is a ALK5 inhibitor with the IC50 of 0.13 μM. ALK5-IN-83 inhibits TGF-β1-induced Smad2 phosphorylation and cell motility in A549 cells .
    ALK5-IN-83
  • HY-151279
    ALK5-IN-30

    		Anaplastic lymphoma kinase (ALK) Cancer
    ALK5-IN-30 (EX-07) is a potent ALK inhibitor, inhibits ALK5 and TGFβ-R1 with both IC50s <10 nM .
    ALK5-IN-30
  • HY-162902
    ALK5-IN-82

    		Others Cardiovascular Disease
    ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis .
    ALK5-IN-82
  • HY-118528
    TP0427736

    		TGF-β Receptor Cancer
    TP0427736 is a selective inhibitor of ALK5 with an IC50 of 2.72 nM. TP0427736 inhibits Smad2/3 phosphorylation in A549 cells. TP0427736 decreases the growth inhibition of human outer root sheath cells .
    TP0427736
  • HY-112877
    ALK-5-IN-1

    		TGF-β Receptor Cancer
    ALK-5-IN-1 is an ALK-5 inhibitor. ALK-5-IN-1 can be used for the research of cancer, and conditions involving fibrosis .
    ALK-5-IN-1
  • HY-142949
    ALK5-IN-7

    		TGF-β Receptor Inflammation/Immunology Cancer
    ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4) .
    ALK5-IN-7
  • HY-142950
    ALK5-IN-6

    		TGF-β Receptor Inflammation/Immunology Cancer
    ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1) .
    ALK5-IN-6
  • HY-111482
    SM 16
    1 Publications Verification

    		 TGF-β Receptor Cardiovascular Disease Inflammation/Immunology Cancer
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
    SM 16
  • HY-18758
    IN-1130
    1 Publications Verification

    		 TGF-β Receptor Inflammation/Immunology Cancer
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
    IN-1130
  • HY-10432A
    A 83-01 sodium
    50+ Cited Publications

    		 Organoid TGF-β Receptor Cancer
    A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively .
    A 83-01 sodium
  • HY-109179A
    Itacnosertib (hydrocholide)

    TP-0184 (hydrocholide)

    		 JAK TGF-β Receptor Cancer
    Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5 .
    Itacnosertib (hydrocholide)
  • HY-13521
    SB-505124
    15+ Cited Publications

    		 TGF-β Receptor Cancer
    SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
    SB-505124
  • HY-13521A
    SB-505124 hydrochloride
    15+ Cited Publications

    		 TGF-β Receptor Cancer
    SB-505124 hydrochloride is a selective inhibitor of?TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with?IC50s?of 129 nM and 47 nM for?ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
    SB-505124 hydrochloride
  • HY-13227
    SD-208
    5+ Cited Publications

    		 TGF-β Receptor Cancer
    SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, and > 100-fold selectivity over TGF-βRII.
    SD-208
  • HY-13012
    RepSox
    15+ Cited Publications

    E-616452; SJN 2511

    		 Organoid TGF-β Receptor Metabolic Disease
    RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes .
    RepSox
  • HY-10432
    A 83-01
    50+ Cited Publications

    		 Organoid TGF-β Receptor Cancer
    A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively .
    A 83-01
  • HY-10327
    GW-6604

    		TGF-β Receptor Metabolic Disease
    GW-6604 is an ALK5 inhibitor with an IC50 value of 140 nM for inhibiting its autophosphorylation, and can be used in the study of liver fibrosis .
    GW-6604
  • HY-12043
    SB 525334
    10+ Cited Publications

    		 TGF-β Receptor Cancer
    SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.
    SB 525334
  • HY-13783
    BIBF0775

    		TGF-β Receptor Cancer
    BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
    BIBF0775
  • HY-109179
    Itacnosertib

    TP-0184

    		 JAK TGF-β Receptor Cancer
    Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871 .
    Itacnosertib
  • HY-18766
    EW-7195

    		TGF-β Receptor p38 MAPK Cancer
    EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung .
    EW-7195
  • HY-78349
    A 77-01
    1 Publications Verification

    		 TGF-β Receptor Cancer
    A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM .
    A 77-01
  • HY-129171
    TGFBR1-IN-1

    		TGF-β Receptor Inflammation/Immunology Cancer
    TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM .
    TGFBR1-IN-1
  • HY-10432R
    A 83-01 (Standard)

    		TGF-β Receptor Cancer
    A 83-01 (Standard) is the analytical standard of A 83-01 (HY-10432). This product is intended for research and analytical applications. A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively .
    A 83-01 (Standard)
  • HY-150169
    THRX-144644

    		TGF-β Receptor Cancer
    THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition .
    THRX-144644
  • HY-10326
    GW788388
    15+ Cited Publications

    		 TGF-β Receptor Cancer
    GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
    GW788388
  • HY-149403
    J-1048

    		Anaplastic lymphoma kinase (ALK) Others
    J-1048 is an activin receptor-like kinase 5 (ALK5) inhibitor. J-1048 can inhibit TAA-induced liver fibrosis in mice by explicitly blocking the TGF-β/Smad signaling pathway .
    J-1048
  • HY-10431
    SB-431542
    Maximum Cited Publications
    194 Publications Verification

    		 Organoid TGF-β Receptor Apoptosis Cancer
    SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
    SB-431542
  • HY-12953
    R-268712

    		TGF-β Receptor TGF-beta/Smad Anaplastic lymphoma kinase (ALK) Cardiovascular Disease Inflammation/Immunology Cancer
    R-268712 is an orally active and selective ALK-5 inhibitor, with an IC50 of 2.5 nM. R-268712 inhibits the phosphorylation of Smad3 in a dose-dependent manner with an IC50 of 10.4 nM. R-268712 suppresses glomerulonephritis as well as glomerulosclerosis by inhibiting TGF-β signaling, which can be used in studies of renal fibrosis and cancer .
    R-268712
  • HY-160237
    HYL001

    		TGF-β Receptor Cancer
    HYL001 (compund 338) is a potent inhibitor of TGFβ receptor 1 (ALK5) that is approximately 9 times more potent than the structurally related compound Galunisertib (HY-13226) and is able to eliminate liver metastases established in mice .
    HYL001
  • HY-103021
    LY3200882
    5+ Cited Publications

    		 TGF-β Receptor Inflammation/Immunology Cancer
    LY3200882 is a potent, highly selective, ATP-competitive and orally active TGF-β receptor type 1 (ALK5) inhibitor with an IC50 of 38.2 nM. LY3200882 inhibits various pro-tumorigenic activities and is also used as an immune modulatory agent .
    LY3200882
  • HY-10431R
    SB-431542 (Standard)

    		Apoptosis TGF-β Receptor Organoid Cancer
    SB-431542 (Standard) is the analytical standard of SB-431542. SB-431542 is a TGF-β receptor kinase inhibitor (TRKI). SB-431542 has inhibitory activity for ALK4, ALK5 and ALK7 with IC50 values of 1 μM, 0.75 μM and 2 μM, respectively. SB-431542 also inhibits TGF-β-induced transcription, gene expression, apoptosis, and growth suppression. SB-431542 can be used for the research of cancer and signal transduction pathways .
    SB-431542 (Standard)
  • HY-12071A
    LDN193189 Tetrahydrochloride
    60+ Cited Publications

    DM-3189 Tetrahydrochloride

    		 Organoid TGF-β Receptor Cancer
    LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM) .
    LDN193189 Tetrahydrochloride
  • HY-13012G
    RepSox

    E-616452; SJN 2511

    		 TGF-β Receptor Metabolic Disease
    RepSox (E-616452) (GMP) is a RepSox (HY-13012) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. RepSox is a potent and selective TGF-β-RI/ALK5 inhibitor .
    RepSox
  • HY-125851
    TP-008

    		TGF-β Receptor Inflammation/Immunology
    TP-008 is a potent, selective and orally active (Activin-Like Kinase 5) ALK5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose .
    TP-008

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