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Type I kinase

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10432
    A 83-01
    Maximum Cited Publications
    129 Publications Verification

    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-13226
    Galunisertib
    65+ Cited Publications

    LY2157299

    TGF-β Receptor Cancer
    Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib
  • HY-117287
    Deucravacitinib
    30+ Cited Publications

    BMS-986165

    JAK STAT Interleukin Related IFNAR Inflammation/Immunology
    Deucravacitinib (BMS-986165) is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation . Deucravacitinib can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus .
    Deucravacitinib
  • HY-P0221
    PACAP (1-38), human, ovine, rat
    5 Publications Verification

    Pituitary Adenylate Cyclase Activating Polypeptide 38

    PACAP Receptor ERK EGFR Reactive Oxygen Species (ROS) Calcium Channel Infection Neurological Disease
    PACAP (1-38), human, ovine, rat is a PAC1 receptor agonist. PACAP (1-38), human, ovine, rat binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively. PACAP (1-38), human, ovine, rat increases the α-secretase activity. PACAP (1-38), human, ovine, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP (1-38), human, ovine, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP (1-38), human, ovine, rat can be used for neurotrophic and neuroprotective research .
    PACAP (1-38), human, ovine, rat
  • HY-10432A
    A 83-01 sodium
    Maximum Cited Publications
    129 Publications Verification

    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-145015

    HM43239

    FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
    Tuspetinib
  • HY-16397
    Phenformin
    5+ Cited Publications

    Phenethylbiguanide

    Mitochondrial Metabolism AMPK Apoptosis Autophagy mTOR Neurological Disease Metabolic Disease Cancer
    Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin inhibits cancer stem cells (CSCs) and possesses potent antitumor potential .
    Phenformin
  • HY-16712
    LDN-214117
    2 Publications Verification

    TGF-β Receptor Cancer
    LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
    LDN-214117
  • HY-108355
    R59949
    1 Publications Verification

    PKC Cancer
    R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
    R59949
  • HY-153268
    Silevertinib
    2 Publications Verification

    BDTX-1535; EGFR-IN-76

    EGFR Infection Neurological Disease Metabolic Disease Cancer
    Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
    Silevertinib
  • HY-18623

    Syk Src Cancer
    VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
    VI 16832
  • HY-12293
    LY2857785
    4 Publications Verification

    CDK Apoptosis Cancer
    LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
    LY2857785
  • 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-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-153701S

    Envudeucitinib; ESK-001

    JAK Interleukin Related IFNAR Isotope-Labeled Compounds Inflammation/Immunology
    Envudeucitinibum (Envudeucitinib) is a highly selective, allosteric and orally active TYK2 inhibitor binding to the JH2 domain of TYK2. Envudeucitinibum has no off-target effects on other kinases (JAK1-3). Envudeucitinibum reduces signaling and production of proinflammatory cytokines including IL-12, IL-23, IL-17, and type I interferons (IFNs). Envudeucitinibum can be used for the research of plaque psoriasis, systemic lupus erythematosus (SLE), and other immune-mediated diseases .
    Envudeucitinibum
  • HY-P10954

    p38 MAPK Others
    Link N peptide is a proteoglycan aggregates activator in the extracellular matrix. Link N peptide can selectively activate the p38 mitogen-activated protein kinase (MAPK) pathway to promote the expression of type I and II collagens in human intervertebral disc cells. Link N peptide is promising for research of intervertebral disc degeneration-related diseases .
    Link N peptide
  • HY-N4119

    Phosphatase Cholinesterase (ChE) p38 MAPK Apoptosis Autophagy Neurological Disease Metabolic Disease
    Neoeriocitrin is a Naringin (HY-N0153) analogue found in Drynaria Rhizome. Neoeriocitrin induces cells proliferation, differentiation, up-regulates type I collagen, osteocalcin, and key osteogenic markers, and increases ALP activity. Neoeriocitrin increases expression of Runx2, COL I, OCN and Beclin1. Neoeriocitrin inhibits phosphorylation of P38 mitogen-activated protein kinase, reduces acetylcholinesterase (AChE) activity, and increases choline acetyltransferase (ChAT) activity. Neoeriocitrin reduces apoptosis and induces autophagy. Neoeriocitrin can be used for the researches of osteoporosis and Alzheimer's disease .
    Neoeriocitrin
  • HY-162266

    Ser/Thr Protease Cancer
    C3TD879 is a Type I kinase inhibitor that potently inhibits CITK catalytic activity (IC50 = 12 nM). C3TD879 binds directly to full-length human CITK in cells (NanoBRET Kd < 10 nM). C3TD879 is a chemical probe suitable for interrogating the complex biology of CITK .
    C3TD879
  • HY-132893

    TAM Receptor Cancer
    AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
    AZ14145845
  • HY-15814

    Bcr-Abl PDGFR c-Kit Src JAK Apoptosis Cancer
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
    HG-7-85-01
  • HY-149665
    BMS-684
    1 Publications Verification

    DGK Cancer
    BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
    BMS-684
  • HY-123450

    Bcr-Abl Apoptosis PDGFR Cancer
    S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    S116836
  • HY-128437
    TGFβ-IN-5
    1 Publications Verification

    TGF-β Receptor Inflammation/Immunology
    TGFβ-IN-5 is a type I transforming growth factor-β receptor (TGF-β R1) kinase inhibitor with an IC50 value of 0.0485 μM. TGFβ-IN-5 reverses the effect of TGF-β-mediated cell activation on the expression of fibrosis-related genes. TGFβ-IN-5 can be used in the research of fibroproliferative diseases .
    TGFβ-IN-5
  • HY-10432R

    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-163572

    PI4P5K Cancer
    PIP5K1α-IN-1 (Compound 3e) is an inhibitor for phosphatidylinositol 4-phosphate 5-kinase type I α (PIP5K1α) with an IC50 of 0.46 μM .
    PIP5K1α-IN-1
  • HY-12083

    Bcr-Abl Cancer
    PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
    PPY-A
  • HY-147342

    Drug Metabolite IMPDH Cancer
    β-Benzamide adenine dinucleotide is a biologically active metabolite of benzamide riboside. β-Benzamide adenine dinucleotide is a competitive inhibitor of human NAD kinase with a Ki value of 90 μM, and inhibits human IMPDH with IC50 values of 0.787 μM and 0.884 μM for type I and type II, respectively. β-Benzamide adenine dinucleotide exhibits inhibitory activities against lactate dehydrogenase, glutamate dehydrogenase, and malate dehydrogenase. β-Benzamide adenine dinucleotide can be used for the study of chronic myelogenous leukemia .
    β-Benzamide adenine dinucleotide
  • HY-137108

    PKA PKG Neurological Disease
    Sp-8-pCPT-cGMPS is a potent cyclic guanosine monophosphate-gated channel agonist and a lipophilic activator of protein kinase G (types I α, I β, and II) and protein kinase A type II with excellent cell membrane permeability and phosphodiesterase stability. Sp-8-pCPT-cGMPS can be used to study the role of cGMP in neural plasticity and synaptic transmission .
    Sp-8-pCPT-cGMPS
  • HY-13012R

    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-13226A

    TGF-β Receptor Cancer
    Galunisertib monohydrate is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib monohydrate
  • HY-119370

    Bcr-Abl Apoptosis Cancer
    CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively .
    CHMFL-ABL-121
  • HY-10364

    Bcr-Abl Cancer
    AP24163 is a BCR-ABL kinase inhibitor. AP24163 inhibits wild-type (native) BCR-ABL and BCR-ABL-T315I with IC50 values of 7 nM and 511 nM, respectively. AP24163 can be used in the research of chronic myeloid leukemia (CML) .
    AP24163
  • HY-13226R

    LY2157299 (Standard)

    TGF-β Receptor Reference Standards Cancer
    Galunisertib (Standard) is the analytical standard of Galunisertib. This product is intended for research and analytical applications. Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
    Galunisertib (Standard)
  • HY-145015A

    HM43239 hydrate

    FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
    Tuspetinib hydrate
  • HY-145015B

    HM43239 dihydrochloride

    FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) dihydrochloride is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib dihydrochloride inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib dihydrochloride inhibits the proliferation and induces the apoptosis of leukemic cells .
    Tuspetinib dihydrochloride
  • HY-W684904

    TGF-β Receptor Cancer
    LY550410 is a small-molecule ATP-competitive inhibitor against type I TGF-β receptor kinase, which contains heteroaryl rings for potent binding to the kinase-domain active site. LY550410 modulates TGF-β signalling, thereby regulates gene expression and ultimately cell growth. LY550410 is promising for research of cancers .
    LY550410
  • HY-137530

    8-Methylamino-cAMP

    PKA Others
    8-MA-cAMP (8-Methylamino-cAMP) is a cyclic AMP analog that acts as a site-selective PKA agonist with similar affinity for the B site of type I and type II protein kinase A. 8-MA-cAMP is used in conjunction with priming analogs that show site A preference, such as 8-piperidinyl cAMP, to achieve selective stimulation of type I .
    8-MA-cAMP
  • HY-E70737

    c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT T670I is a mutant of KIT. KIT T670I Recombinant Human Active Protein Kinase is a recombinant KIT T670I protein that can be used to study KIT T670I-related functions .
    KIT T670I Recombinant Human Active Protein Kinase
  • HY-E70739

    c-Kit Cancer
    KIT (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT V559D/T670I is a mutant of KIT. KIT V559D/T670I Recombinant Human Active Protein Kinase is a recombinant KIT V559D/T670I protein that can be used to study KIT V559D/T670I-related functions .
    KIT V559D/T670I Recombinant Human Active Protein Kinase
  • HY-148827A

    HYBO-165 sodium

    PKA Cancer
    GEM231 sodium is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 sodium induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
    GEM-231 sodium
  • HY-148827

    HYBO-165

    PKA Cancer
    GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
    GEM-231
  • HY-131777

    PKA Others
    2-Cl-cAMP is an analog of cAMP and a potent stimulator of cAMP-dependent protein kinases such as PKA type I and II. 2-Cl-cAMP can be used as starting material for cyclic nucleotides .
    2-Cl-cAMP
  • HY-114192

    TGF-β Receptor Cancer
    TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
    TGFβRI-IN-1
  • HY-E70834

    JAK Cancer
    JAK1 is a non-receptor tyrosine kinase that plays a critical role in cell signaling via type I/II cytokines and interferons (IFNs). JAK1(JH1) is a kinase domain. JAK1(JH1) Recombinant Human Active Protein Kinase is a recombinant JAK1(JH1) protein that can be used to study JAK1(JH1)-related functions .
    JAK1(JH1) Recombinant Human Active Protein Kinase
  • HY-174665

    mRNA Cancer
    Human IFNAR2 mRNA encodes the human interferon alpha and beta receptor subunit 2 (IFNAR2) protein, a protein that belongs to the type II cytokine receptor family. IFNAR2 is a type I membrane protein that forms one of the two chains of a receptor for interferons alpha and beta. Binding and activation of the receptor stimulates Janus protein kinases, which in turn phosphorylate several proteins, including STAT1 and STAT2.
    Human IFNAR2 mRNA
  • HY-W707119

    E-616452 hydrochloride; SJN 2511 hydrochloride

    TGF-beta/Smad Anaplastic lymphoma kinase (ALK) Metabolic Disease
    RepSox hydrochloride is a potent and selective inhibitor of transforming growth factor-β receptor I/activin-like kinase 5 (TGF-β-RI/ALK5). RepSox hydrochloride inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox hydrochloride can be used in the study of obesity and related metabolic diseases such as type 2 diabetes.
    RepSox hydrochloride
  • 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-137628

    PKA Cancer
    Sp-8-PIP cAMP sodium is a non-corresponding isomer of 8-Piperidino-cAMP. 8-Piperidino-cAMP binds with high affinity to site A of the regulatory subunit of cAMP-dependent protein kinase type I (AI). Sp-8-PIP cAMP sodium can be used as an antagonist of cAMP-induced activation .
    Sp-8-PIP cAMP
  • HY-164469

    Bcr-Abl Apoptosis STAT Cancer
    CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
    CHMFL-48

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