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Targets Recommended: ALK

Results for "ALK Inhibitors" in MCE Product Catalog:

94

Inhibitors & Agonists

1

Screening Libraries

1

Natural
Products

7

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-131244
    ALK-IN-9

    ALK Cancer
    ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively.
  • HY-128596
    ALK-IN-6

    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.
  • HY-112815
    ALK2-IN-2

    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.
  • HY-128569
    ALK-IN-5

    ALK Neurological Disease
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
  • HY-15358
    ALK inhibitor 2

    ALK Cancer
    ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.
  • HY-15357
    ALK inhibitor 1

    ALK Cancer
    ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.
  • HY-13464
    ALK-IN-1

    Brigatinib analog

    ALK Cancer
    ALK-IN-1 (Brigatinib analog) is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.
  • HY-130794
    ALK/ROS1-IN-1

    ALK ROS Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
  • HY-111752
    EML4-​ALK kinase inhibitor 1

    ALK Cancer
    EML4-ALK kinase inhibitor 1 is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.
  • HY-15656S
    Ceritinib D7

    LDK378 D7

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.
  • HY-15609
    AZD-3463

    ALK/IGF1R inhibitor

    ALK IGF-1R Autophagy Cancer Endocrinology
    AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.
  • HY-123919
    TL13-112

    PROTAC ALK Cancer
    TL13-112 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.14 nM. TL13-112 also prompts the degradation of additional kinases including Aurora A, FER, PTK2 and RPS6KA1 with IC50 values of 8550 nM, 42.4 nM, 25.4 nM, and 677 nM, respectively. TL13-112 is comprised of the conjugation of Ceritinib (HY-15656) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-122582
    TL13-12

    PROTAC ALK Cancer
    TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the cereblon ligand of Pomalidomide (HY-10984).
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-12273
    DMH-1

    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.
  • HY-111482
    SM 16

    TGF-β Receptor Cancer Inflammation/Immunology Cardiovascular Disease
    SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.
  • HY-10432A
    A 83-01 sodium salt

    TGF-β Receptor ALK Cancer
    A 83-01 sodium salt 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.
  • HY-13521
    SB-505124

    TGF-β Receptor Cancer
    SB-505124 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.
  • HY-13521A
    SB-505124 hydrochloride

    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.
  • HY-12274
    ML347

    LDN 193719

    TGF-β Receptor Cancer
    ML347(DN193719) is a highly selective ALK1/ALK2 inhibitor with IC50s of 46/32 nM; shows >300-fold selectivity for ALK2 vs.
  • HY-10432
    A 83-01

    ALK 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.
  • HY-112140
    JH-VIII-157-02

    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.
  • HY-112156
    MS4077

    PROTAC ALK Cancer
    MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 37 nM for binding affinity to ALK.
  • HY-112155
    MS4078

    PROTAC ALK Cancer
    MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK.
  • HY-12071
    LDN193189

    DM-3189

    TGF-β Receptor Cancer
    LDN193189 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).
  • HY-13012
    RepSox

    E-616452; SJN 2511

    TGF-β Receptor Cancer
    RepSox is a potent and selective of the TGFβR-1/ALK5 inhibitor which inhibits ALK5 autophosphorylation with IC50 of 4 nM.
  • HY-12071A
    LDN193189 Tetrahydrochloride

    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).
  • HY-12278
    K02288

    TGF-β Receptor Others
    K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
  • HY-15897
    LDN-212854

    TGF-β Receptor Cancer
    LDN-212854 is a novel BMP inhibitor that exhibits substantially greater selectivity for BMP versus the TGF-β type I receptors; possesses a bias towards ALK2(IC50=1.3 nM) versus ALK1 and ALK3 compared to other inhibitors.
  • HY-112801
    F-1

    ALK ROS Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively.
  • HY-17603
    Belizatinib

    TSR-011

    ALK Trk Receptor Cancer
    Belizatinib is an oral, dual, potent inhibitor of ALK and TRKA, TRKB, and TRKC, with IC50 of 0.7 nM for wild-type recombinant ALK kinase.
  • HY-12215
    Lorlatinib

    PF-06463922

    ALK ROS Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib has anticancer activity.
  • HY-135887
    ZX-29

    ALK Apoptosis Autophagy Cancer
    ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect.
  • HY-13418
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 dihydrochloride

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
  • HY-13418A
    Dorsomorphin

    Compound C; BML-275

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
  • HY-10431
    SB-431542

    TGF-β Receptor Cancer
    SB-431542 is a potent and selective inhibitor of ALK5/TGF-β type I Receptor with an IC50 value of 94 nM.
  • HY-19628
    OD36

    RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM.
  • HY-15841
    CEP-37440

    ALK FAK Cancer
    CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).
  • HY-16712
    LDN-214117

    TGF-β Receptor Cancer
    LDN-214117 is a potent and selective ALK2 inhibitor with IC50 of 22 nM; > 100 fold selectivity for ALK5; also inhibits BMP6(IC50=100 nM).
  • HY-13227
    SD-208

    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.
  • HY-19928A
    Vactosertib Hydrochloride

    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.
  • HY-19928
    Vactosertib

    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.
  • HY-18758
    IN-1130

    TGF-β Receptor Cancer Inflammation/Immunology
    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.
  • HY-12331
    KRCA-0008

    Ack1 ALK Cancer
    KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.
  • HY-13011
    Alectinib

    CH5424802; RO5424802; AF802

    ALK Cancer
    Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-10192
    NVP-TAE 684

    TAE 684

    ALK Apoptosis Cancer
    NVP-TAE 684 (TAE 684) is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-136195
    TL13-110

    ALK Cancer
    TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
  • HY-136194
    TL13-22

    ALK Cancer
    TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
  • HY-13011A
    Alectinib Hydrochloride

    CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride

    ALK Cancer
    Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration.
  • HY-122856
    AZ12601011

    TGF-β Receptor Cancer
    AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
  • HY-13326
    ASP3026

    ALK Cancer
    ASP3026 is a novel and selective inhibitor for ALK (anaplastic lymphoma kinase) with IC50 of 3.5 nM.
  • HY-15801
    HG-14-10-04

    ALK Cancer
    HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.
  • HY-12953
    R-268712

    TGF-β Receptor Cancer
    R-268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.
  • HY-12678
    Entrectinib

    NMS-E628; RXDX-101

    ROS Trk Receptor ALK Autophagy Cancer
    Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • 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.
  • HY-12043
    SB 525334

    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.
  • HY-12857
    Brigatinib

    AP-26113

    ALK Cancer
    Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC50 of 0.6 nM.
  • HY-103714A
    Ensartinib hydrochloride

    X-396 hydrochloride

    ALK c-Met/HGFR Cancer
    Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-103714
    Ensartinib

    X-396

    ALK c-Met/HGFR Cancer
    Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
  • HY-111416
    WY-135

    ALK ROS Cancer
    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • 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.
  • HY-18030A
    CEP-28122 mesylate salt

    ALK Cancer
    CEP-28122 mesylate salt is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
  • HY-18030
    CEP-28122

    ALK Cancer
    CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.
  • HY-78349
    A 77-01

    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.
  • HY-50878
    Crizotinib

    PF-02341066

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
  • HY-10326
    GW788388

    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.
  • HY-13020
    GSK1838705A

    ALK IGF-1R Insulin Receptor Cancer Endocrinology
    GSK1838705A is a potent and reversible IGF-IR and the insulin receptor inhibitor with IC50s of 2.0 and 1.6 nM, respectively. It also inhibits ALK with an IC50 of 0.5 nM.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-129171
    TGFBR1-IN-1

    TGF-β Receptor Cancer Inflammation/Immunology
    TGFBR1-IN-1 is an ALK5 inhibitor extracted from patent WO2018004290A1, Compound 33, has an IC50 of 10-100 nM.
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-50878A
    Crizotinib hydrochloride

    PF-02341066 hydrochloride

    ALK c-Met/HGFR ROS Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
  • HY-109084
    Conteltinib

    CT-707

    FAK Cancer
    Conteltinib (CT-707) is a multi-kinase inhibitor targeting FAK, ALK, and Pyk2. Conteltinib (CT-707) exerts significant inhibitory effect on FAK with an IC50 of 1.6 nM.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-103021
    LY3200882

    TGF-β Receptor Cancer Inflammation/Immunology
    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.
  • HY-16590
    X-376

    ALK c-Met/HGFR Cancer
    X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC50=0.61 nM). X-376 is a less potent inhibitor of MET (IC50=0.69 nM). X-376 displays potent anti-tumor activity.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-100375
    Diroximel fumarate

    ALKS 8700; BIIB098

    Others Others
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) prodrug in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS).
  • HY-125851
    TGFβRI-IN-2

    ALK Inflammation/Immunology
    TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 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.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-15656A
    Ceritinib dihydrochloride

    LDK378 dihydrochloride

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib dihydrochloride (LDK378 dihydrochloride) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib dihydrochloride (LDK378 dihydrochloride) shows great antitumor potency.
  • HY-103022
    Repotrectinib

    TPX-0005

    ROS Trk Receptor ALK Cancer
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity.
  • HY-15656
    Ceritinib

    LDK378

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • 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.
  • HY-N4126
    6-Demethoxytangeretin

    ALK Cancer Inflammation/Immunology Neurological Disease
    6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa. 6-Demethoxytangeretin exerts anti-inflammatory activity and anti-allergic activity, suppresses production and gene expression of interleukin-6 in human mast cell-1 via anaplastic lymphoma kinase (ALK) and mitogen-activated protein kinase (MAPK) pathways. 6-Demethoxytangeretin facilitates the CRE-mediated transcription associated with learning and memory in cultured hippocampal neurons.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.