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ALK Inhibitors

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183

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151289

    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-157391

    ROS Kinase Anaplastic lymphoma kinase (ALK) Cancer
    ALK/ROS1-IN-3 (compound C01) is a ROS1 and ALK dual inhibitor with IC50s of 42.3 nM and 49.1 nM for ROS1 G2032R and ALK G1202R, respectively .
    ALK/ROS1-IN-3
  • HY-146408

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-21 (Compound B10), a potent ALK inhibitor for ALKG1202R mutation, exhibits remarkable enzymatic inhibitory potency with IC50 values of 4.59 nM, 2.07 nM and 5.95 nM toward ALK WT, ALK L1196M and ALK G1202R, respectively. ALK-IN-21 efficiently inhibits the proliferation of ALK-positive Karpas299 and H2228 cells both with IC50 values of 0.07 μM. ALK-IN-21 can be used for the research of anaplastic large cell lymphoma .
    ALK-IN-21
  • HY-18030B

    Anaplastic lymphoma kinase (ALK) Others
    CEP-28122 mesylate hydrochloride is a diaminopyrimidine derivative.CEP-28122 mesylate hydrochloride is a potent, selective, and orally bioavailable ALK inhibitor with an IC50 of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor and good pharmacokinetic activity .
    CEP-28122 mesylate hydrochloride
  • HY-151273

    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-151270

    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-151272

    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-153246

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor. ALK2-IN-5 can inhibit ALK2 activity and FGFR activity. ALK2-IN-5 can be used for the research of disorders associated with ALK2 activity and/or FGFR activity, such as cancer .
    ALK2-IN-5
  • HY-112877

    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-151277

    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-12273
    DMH-1
    5+ Cited Publications

    Autophagy TGF-β Receptor Cancer
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
    DMH-1
  • HY-151275

    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

    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-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-151282

    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-144437

    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-12273R

    Autophagy TGF-β Receptor Cancer
    DMH-1 (Standard) is the analytical standard of DMH-1. DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
    DMH-1 (Standard)
  • HY-151283

    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-144043

    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-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-151279

    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-161662

    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-12071A
    LDN193189 Tetrahydrochloride
    55+ 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-155227

    Anaplastic lymphoma kinase (ALK) EGFR Apoptosis Cancer
    ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
    ALK/EGFR-IN-1
  • HY-147833

    Anaplastic lymphoma kinase (ALK) Apoptosis Cancer
    ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALK L1196M and ALK G1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research .
    ALK-IN-22
  • HY-10432A
    A 83-01 sodium
    45+ 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-12215
    Lorlatinib
    25+ Cited Publications

    PF-06463922

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib
  • HY-135509

    PF-06463922 acetate

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib acetate
  • HY-168607

    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-128596

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively .
    ALK-IN-6
  • HY-151155

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
    ALK-IN-23
  • HY-111752

    Anaplastic lymphoma kinase (ALK) Cancer
    EML4-ALK kinase inhibitor 1 is a potent orally active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM .
    EML4-ALK kinase inhibitor 1
  • HY-112140

    Anaplastic lymphoma kinase (ALK) Cancer
    JH-VIII-157-02 is a structural analogue of alectinib, acts as an ALK inhibitor, and shows an IC50 of 2 nM for echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) G1202R in cells.
    JH-VIII-157-02
  • HY-12215R

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib (Standard)
  • HY-163507

    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-156432

    Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase Cancer
    ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .
    ALK-IN-26
  • HY-151233

    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-112815
    ALK2-IN-2
    1 Publications Verification

    TGF-β Receptor Cancer
    ALK2-IN-2 is a potent and selective inhibitor of activin receptor-like kinase 2 (ALK2) with an IC50 of 9 nM, and over 700-fold selectivity against ALK3 .
    ALK2-IN-2
  • HY-155227B

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC50s of 0.1360, 0.0332, and 0.0339 μM, respectively .
    ALK/EGFR-IN-3
  • HY-12274
    ML347
    5+ Cited Publications

    LDN 193719

    TGF-β Receptor Cancer
    ML347 (LDN193719) is a highly selective ALK1/ALK2 inhibitor. ML347 has IC50 values of 46 and 32 nM against ALK1 and ALK2, respectively, >300-fold selective over ALK3. ML347 block the phosphorylation of Smad1/5 by TGF-β1 .
    ML347
  • HY-10432
    A 83-01
    45+ 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-160520

    Anaplastic lymphoma kinase (ALK) Cancer
    ALK-IN-28 (compound 22) is an inhibitor of anaplastic lymphoma kinase (ALK) .
    ALK-IN-28
  • HY-136773

    ALK2-IN-4

    TGF-β Receptor Metabolic Disease
    ALK2-IN-4 is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base .
    KER047
  • HY-162902

    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-109179A

    TP-0184 (hydrocholide)

    JAK TGF-β Receptor Cancer
    Itacnosertib hydrocholide is an inhibitor of JAK2, ACVR1 (ALK2) and ALK5 .
    Itacnosertib (hydrocholide)
  • HY-136773A

    ALK2-IN-4 succinate

    TGF-β Receptor Metabolic Disease
    ALK2-IN-4 succinate is a potent ALK2 inhibitor extracted from patent WO2020086963A1, compound Formula I free base .
    KER047 succinate
  • HY-148234

    Anaplastic lymphoma kinase (ALK) Cancer
    M4K2234 (compound 26b) is an ALK2 inhibitor. M4K2234 inhibits ALK2 and ALK5 with IC50s of 5 and 2144 nM, respectively. M4K2234 can be used as a chemical probe for ALK1 and ALK2 protein kinases. M4K2234 can be used for the research of cancer .
    M4K2234
  • HY-153386

    Anaplastic lymphoma kinase (ALK) Cancer
    CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
    CPD-1224
  • HY-144732

    Trk Receptor Anaplastic lymphoma kinase (ALK) Cancer
    TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC50 values of 2.2, 9.3 and 38 nM towards TRKA, ALK WT and ALK L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases .
    TRK/ALK-IN-1

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