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ALK5 Inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10431
    SB-431542
    Maximum Cited Publications
    294 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-10432
    A 83-01
    125+ 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-13012
    RepSox
    20+ 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-12043
    SB 525334
    15+ 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-19928
    Vactosertib
    5+ Cited Publications

    EW-7197; TEW-7197

    		 TGF-β Receptor Cancer
    Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect .
    Vactosertib
  • HY-10432A
    A 83-01 sodium
    125+ 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-13521
    SB-505124
    20+ 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-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-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-103021
    LY3200882
    10+ 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-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-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-168990
    Ontunisertib

    AGMB-129

    		 TGF-β Receptor Metabolic Disease Inflammation/Immunology Cancer
    Ontunisertib (AGMB-129) is an orally active and selective gastrointestinal-restricted ALK5 (TGFβR1) inhibitor. Ontunisertib blocks signalling of the pro-fibrotic TGFβ pathway. Ontunisertib can be used for the research of fibrostenotic Crohn’s disease .
    Ontunisertib
  • HY-172240
    Tosposertib

    TU2218 free base

    		 Anaplastic lymphoma kinase (ALK) VEGFR Inflammation/Immunology Cancer
    Tosposertib (TU2218 free base) is an ALK5/VEGFR2 dual inhibitor (IC50 = 1.2 nM/4.9 nM). Tosposertib directly restores the activity of damaged cytotoxic T lymphocytes (CTLs) and natural killer cells inhibited by TGFβ and suppresses the activity and viability of regulatory T cells. Tosposertib can be used for the study of melanoma and colon cancer .
    Tosposertib
  • HY-19928A
    Vactosertib Hydrochloride
    5+ Cited Publications

    EW-7197 Hydrochloride; TEW-7197 Hydrochloride

    		 TGF-β Receptor Cancer
    Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect .
    Vactosertib Hydrochloride
  • HY-111482
    SM 16
    5 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-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-18766
    EW-7195
    1 Publications Verification

    		 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
    2 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-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-10431R
    SB-431542 (Standard)

    		Apoptosis TGF-β Receptor Organoid Reference Standards 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-117887
    Fidrisertib

    BLU-782; IPN-60130; ALK2-IN-1

    		 TGF-β Receptor Cancer
    Fidrisertib (BLU-782) is the orally active inhibitor for activin receptor-like kinase 2 (ALK2) that inhibits ALK2 R206H, ALK2, ALK1, ALK6, ALK3, ALK4, TGFβR2 and ALK5 with IC50s of 0.2, 0.6, 3, 24, 45, 65, 67 and 155 nM, respectively .
    Fidrisertib
  • 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-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-N4107
    Phyllanthin
    1 Publications Verification

    		 TGF-beta/Smad Infection Inflammation/Immunology Cancer
    Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
    Phyllanthin
  • 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-N1510
    Kaempferol 3-O-gentiobioside

    		Glycosidase Notch Toll-like Receptor (TLR) NF-κB Mucin Reactive Oxygen Species (ROS) Bacterial TGF-beta/Smad Anaplastic lymphoma kinase (ALK) Infection Inflammation/Immunology Cancer
    Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer .
    Kaempferol 3-O-gentiobioside
  • HY-13521A
    SB-505124 hydrochloride
    20+ 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-135366
    HPN-01

    		IKK Inflammation/Immunology
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2 .
    HPN-01
  • HY-10432R
    A 83-01 (Standard)

    		Reference Standards 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-137918
    TGF-βRI inhibitor 3

    		Src TGF-β Receptor Anaplastic lymphoma kinase (ALK) Others
    TGF-βRI inhibitor 3 (Compound 9ac) is a selective TGF-β inhibitor. TGF-βRI inhibitor 3 can effectively inhibit the TGF-β signaling pathway. TGF-βRI inhibitor 3 has IC50 values of 13 μM and 0.63 μM for c-Src kinase and ALK5 kinase, respectively .
    TGF-βRI inhibitor 3
  • HY-125851
    TP-008

    		TGF-β Receptor Inflammation/Immunology
    TP-008, a chemical probe, 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
  • 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) 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 .
    ALK5-IN-28
  • HY-118528A
    TP0427736 hydrochloride
    2 Publications Verification

    		 TGF-β Receptor Endocrinology
    TP0427736 hydrochloride is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50=836 nM). TP0427736 hydrochloride also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. TP0427736 hydrochloride can be used for the research of androgenic alopecia (AGA) .
    TP0427736 hydrochloride
  • 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-178231
    ALK5-IN-85

    		TGF-β Receptor Inflammation/Immunology Cancer
    ALK5-IN-85 (Compound 19) is a TGFβRI (ALK5) inhibitor with an IC50 < 100 ?nM. ALK5-IN-85 can be used for respiratory diseases including idiopathic pulmonary fibrosis, asthma, COPD and lumg cancer, and dermal and ocular fibrotic conditions research .
    ALK5-IN-85
  • 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-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-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-13012R
    RepSox (Standard)

    E-616452 (Standard); SJN 2511 (Standard)

    		 Organoid TGF-β Receptor Reference Standards Metabolic Disease
    RepSox (Standard) is the analytical standard of RepSox. This product is intended for research and analytical applications. 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 (Standard)
  • 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

    		Anaplastic lymphoma kinase (ALK) 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-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-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

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