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Targets Recommended: Ser/Thr Protease SRPK

Results for "(-)-Serine" in MCE Product Catalog:

81

Inhibitors & Agonists

4

Screening Libraries

1

Dye Reagents

10

Peptides

2

MCE Kits

13

Natural
Products

9

Recombinant Proteins

Cat. No. Product Name Target Research Areas
  • HY-N0650
    L-Serine

    (-)-Serine; (S)-Serine

    Endogenous Metabolite Cancer
    L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-Y0507
    DL-Serine

    Others Cancer Infection
    DL-Serine, a fundamental metabolite, is a mixture of D-Serine and L-Serine. DL-Serine has antiviral activity against the multiplication of tobacco mosaic virus (TMV).
  • HY-15129
    O-Phospho-L-serine

    L-Serine O-phosphate; L-SOP

    mGluR Endogenous Metabolite Neurological Disease
    O-Phospho-L-serine is the immediate precursor to L-serine in the serine synthesis pathway, and an agonist at the group III mGluR receptors (mGluR4, mGluR6, mGluR7, and mGluR8); O-Phospho-L-serine also acts as a weak antagonist for mGluR1 and a potent antagonist for mGluR2.
  • HY-136276
    DMNB-caged-Serine

    Others Others
    DMNB-caged-Serine photoactivates to release serine by visible blue light (405 nm) in cells. DMNB can be incorporated into S.cerevisiae proteins when introduces into growth medium at millimolar concentrations.
  • HY-100808
    (R)-Serine

    iGluR Endogenous Metabolite Others
    (R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. (R)-Serine has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
  • HY-101409A
    O-Acetyl-L-serine hydrochloride

    Endogenous Metabolite Metabolic Disease
    O-Acetyl-L-serine hydrochloride is an endogenous metabolite.
  • HY-101409
    O-Acetylserine

    O-Acetyl-L-Serine

    Endogenous Metabolite Others
    O-Acetylserine (O-Acetyl-L-serine) is an intermediate in the biosynthesis of the amino acid cysteine in bacteria and plants.
  • HY-18522
    AA26-9

    Phospholipase Metabolic Disease
    AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
  • HY-B0385
    Gabexate mesylate

    FOY

    Factor Xa Proteasome Inflammation/Immunology
    Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
  • HY-113013
    Hydroxypyruvic acid

    β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid

    Endogenous Metabolite Metabolic Disease
    Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
  • HY-100012
    CBR-5884

    Others Cancer
    CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
  • HY-15130
    DL-O-Phosphoserine

    Endogenous Metabolite Metabolic Disease
    DL-O-Phosphoserine, a normal metabolite in human biofluid, is an ester of serine and phosphoric acid.
  • HY-113013A
    Hydroxypyruvic acid lithium hydrate

    β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate

    Endogenous Metabolite Metabolic Disease
    Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
  • HY-12821
    AEBSF hydrochloride

    Thrombin Influenza Virus Others
    AEBSF hydrochloride is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.
  • HY-B0496
    PMSF

    Phenylmethylsulfonyl fluoride; Benzylsulfonyl fluoride

    Cathepsin Others
    PMSF is an irreversible serine/cysteine protease inhibitor commonly used in the preparation of cell lysates.
  • HY-U00282
    Chymase-IN-2

    Others Inflammation/Immunology
    Chymase-IN-2 is a chymase modulator which is useful in the treatment of inflammatory and serine protease mediated disorders.
  • HY-119759
    Lipoxamycin

    Fungal Infection
    Lipoxamycin is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • HY-117661
    SPHINX31

    SRPK Cancer
    SPHINX31 is a potent and selective inhibitor of serine/arginine-rich protein kinase 1 (SRPK1), with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 is a potential topical therapeutic for neovascular eye disease.
  • HY-119759A
    Lipoxamycin hemisulfate

    Fungal Infection
    Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • HY-13949
    SRPIN340

    SRPK inhibitor

    SRPK Virus Protease Cancer
    SRPIN340 is an ATP-competitive serine-arginine-rich protein kinase (SRPK) inhibitor, with a Ki of 0.89 μM for SRPK1.
  • HY-U00346
    DPP-IV-IN-1

    Dipeptidyl Peptidase Metabolic Disease
    DPP-IV-IN-1 is a potent inhibitor of dipeptidyl peptidase IV (DPP-IV), a highly specific serine protease, with an IC50 of 4.6 nM.
  • HY-112654
    GCN2iB

    Eukaryotic Initiation Factor (eIF) Autophagy Cancer
    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
  • HY-129651
    SHMT-IN-1

    Others Cancer
    SHMT-IN-1 (compound (±)-46) is a potent inhibitor of plasmodial serine hydroxymethyltransferase (SHMT). SHMT-IN-1 has antitumor activity.
  • HY-16511
    Upamostat

    WX-671

    Ser/Thr Protease PAI-1 Cancer
    Upamostat (WX-671) is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
  • HY-33900
    Dihydrofuran-3(2H)-one

    3-Oxotetrahydrofuran

    Others Others
    Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.
  • HY-B0919
    Azaserine

    CI-337; O-Diazoacetyl-L-Serine; P-165

    Bacterial Antibiotic Cancer Infection
    Azazerine (CI-337) is a competitive inhibitor of glutamine amidotransferase, a key enzyme responsible for glutamine metabolism.
  • HY-50683
    JNJ-38877605

    c-Met/HGFR Cancer
    JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
  • HY-111866
    PROTAC RIPK degrader-2

    PROTAC RIP kinase Inflammation/Immunology
    PROTAC RIPK degrader-2 is a nonpeptidic PROTAC which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
  • HY-114164
    Thrombin

    Thrombin Neurological Disease
    Thrombin is a trypsin-like allosteric serine protease. Thrombin enables site-specific cleavage of fusion proteins with an accessible Thrombin recognition sequence and can be used to digest GST-tagged proteins.
  • HY-112066
    SHIN1

    RZ-2994

    Others Cancer
    SHIN1 (RZ-2994) is a human serine hydroxymethyltransferse 1 and 2 (SHMT1/2) inhibitor with IC50s of 5 and 13 nM, respectively, in an in vitro assay.
  • HY-P1746A
    Protein Kinase C (19-31) (TFA)

    PKC (19-31) (TFA)

    PKC Inflammation/Immunology
    Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
  • HY-P1746
    Protein Kinase C (19-31)

    PKC (19-31)

    PKC Inflammation/Immunology
    Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
  • HY-13802
    SC-514

    GK 01140

    IKK Cancer
    SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
  • HY-108717
    Protease K

    Others Others
    Protease K is a nonspecific serine protease that is useful for general digestion of proteins. Protease K is active in the presence of SDS or urea and over a wide range of pH (4-12), salt concentrations, and temperatures.
  • HY-W018781
    Benzamidine hydrochloride

    Ser/Thr Protease Cancer
    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 µM, 21 µM, 20 µM and 110 µM for uPA, trypsin, tryptase and factor Xa, respectively.
  • HY-136069
    QPX7728

    Bacterial Infection
    QPX7728 is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. QPX7728 inhibits key serine and metallo beta-lactamases at a nano molar range.
  • HY-P1113
    Phospho-Glycogen Synthase Peptide-2(substrate)

    GSK-3 Others
    Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases.
  • HY-P1113A
    Phospho-Glycogen Synthase Peptide-2(substrate) TFA

    GSK-3 Others
    Phospho-Glycogen Synthase Peptide-2 (substrate) is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used for affinity purification of protein-serine kinases.
  • HY-117240
    NCT-502

    Others Cancer
    NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.
  • HY-10865
    LY2183240

    FAAH Autophagy Neurological Disease
    LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the EC-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
  • HY-P0219
    Microcystin-LA

    Phosphatase Cancer
    Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
  • HY-137552
    MKI-1

    MASTL Kinase Inhibitor-1

    Others Cancer
    MKI-1, an inhibitor of MASTL (microtubule-associated serine/threonine kinase-like) with an IC50 of 9.9 μM, exerts antitumor and radiosensitizer activities through PP2A activation in breast cancer.
  • HY-B0190A
    Nafamostat mesylate

    FUT-175

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease Cancer
    Nafamostat mesylate, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat mesylate supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat mesylate blocks activation of SARS-CoV-2..
  • HY-B0190
    Nafamostat

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat blocks activation of SARS-CoV-2.
  • HY-B0190B
    Nafamostat hydrochloride

    Ser/Thr Protease Apoptosis SARS-CoV Cardiovascular Disease
    Nafamostat hydrochloride, a synthetic serine protease inhibitor, is an anticoagulant. Nafamostat hydrochloride supresses T cell auto-reactivity by decreasing granzyme activity and CTL cytolysis. Nafamostat hydrochloride blocks activation of SARS-CoV-2..
  • HY-114492
    GSK547

    GSK'547

    RIP kinase Cancer
    GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-128918
    SIS17

    HDAC Others
    SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
  • HY-136433
    N,N'-Dinitrosopiperazine

    1,4-Dinitrosopiperazine; DNP

    Others Cancer
    N,N'-Dinitrosopiperazine (1,4-Dinitrosopiperazine; DNP) is a carcinogen with specificity for nasopharyngeal epithelium and facilitates NPC metastasis. N,N'-Dinitrosopiperazine regulates multiple signaling pathways through protein phosphorylation, including LYRIC at serine 568.
  • HY-18081
    PF 750

    FAAH Autophagy Metabolic Disease
    PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile.
  • HY-114492A
    (Rac)-GSK547

    RIP kinase Cancer
    (Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-I1070
    D-Isoleucine

    (R)-Isoleucine

    Others Neurological Disease
    D-Isoleucine ((R)-Isoleucine), an isoleucine stereoisomer, is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine.
  • HY-126973
    BI-1230

    HCV Protease Infection
    BI-1230 is potent and digit nanomolar inhibitor of HCV NS3 protease and of viral replication. BI-1230 is also highly selective against other serine/cysteine proteases. BI-1230 shows good Pharmacokinetic(PK) activity.
  • HY-13512
    Camostat mesylate

    Camostat mesilate; FOY305; FOY-S980

    Ser/Thr Protease SARS-CoV Infection Inflammation/Immunology
    Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.
  • HY-110148
    WWL113

    Others Metabolic Disease
    WWL113 is a selective and orally active Ces3 and Ces1f inhibitor, with IC50 values of 120 nM and 100 nM for Ces3 and Ces1f, respectively. WWL113 appears to show excellent selectivity for the 60-kDa serine hydrolase (or hydrolases).
  • HY-126254
    BI-4924

    Others Cancer
    BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
  • HY-15358
    ALK inhibitor 2

    ALK FAK Cancer
    ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
  • HY-130515
    Cdc7-IN-3

    CDK Cancer
    Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-15357
    ALK inhibitor 1

    ALK FAK Cancer
    ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
  • HY-130516
    Cdc7-IN-4

    CDK Cancer
    Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-N1996
    Chebulagic acid

    COX Lipoxygenase SARS-CoV Influenza Virus Infection Inflammation/Immunology
    Chebulagic acid is a COX-LOX dual inhibitor isolated from the fruits of Terminalia chebula Retz, on angiogenesis. Chebulagic acid is a M2 serine to asparagine 31 mutation (S31N) inhibitor and influenza antiviral. Chebulagic acid also against SARS-CoV-2 viral replication with an EC50 of 9.76 μM.
  • HY-130519
    Cdc7-IN-7

    CDK Cancer
    Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
  • HY-18977
    KML29

    MAGL Metabolic Disease Inflammation/Immunology
    KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
  • HY-11091
    Razaxaban hydrochloride

    BMS 561389 hydrochloride; DPC 906 hydrochloride

    Factor Xa Thrombin Cardiovascular Disease
    Razaxaban hydrochloride (BMS 561389 hydrochloride) is a highly potent, selective and orally active factor Xa inhibitor with a Ki of 0.19 nM. Razaxaban hydrochloride exhibits excellent selectivity (>5000-fold) for factor Xa over other related serine proteases. Razaxaban hydrochloride is also a potent thrombin inhibitor with a Ki of 540 nM. Razaxaban hydrochloride has strongly antithrombotic activity.
  • HY-14380
    PF-3845

    FAAH Autophagy Inflammation/Immunology Cancer
    PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
  • HY-100415
    UKI-1

    UKI-1C

    PAI-1 Ser/Thr Protease Infection Cancer
    UKI-1 (UKI-1C) is a potent urokinase-type plasminogen activator (uPA) inhibitor with a Ki of 0.41 μM. UKI-1 is also a low molecular weight serine protease inhibitor. UKI-1 is a potent antimetastatic agent and inhibits the invasive capacity of carcinoma cells.
  • HY-N6785
    Okadaic acid

    Phosphatase Parasite Apoptosis Infection
    Okadaic acid is extracted from black sponges of the genus Halichondria. Okadaic acid is a non-comepetitive, selective and reversible serine/threonine-specific protein phosphatases 1 (PP1), PP2A and PP3 inhibitor with IC50s of 10-15 nM, 0.5 nM and 4 nM, respectively. Okadaic acid eliminate metazoan symbionts/parasites by apoptosis.
  • HY-10300
    Narlaprevir

    SCH 900518

    HCV HCV Protease Infection
    Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir (SCH 900518) also inhibits the hepatitis C virus (HCV) nonstructural protein 3 serine protease. Narlaprevir (SCH 900518) can be used for chronic hepatitis C research.
  • HY-16576A
    (Z)-SMI-4a

    Pim Cancer
    (Z)-SMI-4a is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 µM. (Z)-SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. (Z)-SMI-4a has anticancer activity.
  • HY-11107
    PHA-665752

    c-Met/HGFR Autophagy Apoptosis Cancer
    PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity.
  • HY-116815
    Lalistat 1

    Bacterial Infection Neurological Disease
    Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease.
  • HY-103463
    SA57

    FAAH MAGL Neurological Disease
    SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases.
  • HY-10524
    GSK1904529A

    IGF-1R Insulin Receptor Apoptosis Cancer Endocrinology
    GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
  • HY-128570
    FD-IN-1

    Complement System Inflammation/Immunology
    FD-IN-1 (Compound 12) is an orally bioavailable and selective factor D (FD) inhibitor with an IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5 µM, respectively.
  • HY-N6798
    Myriocin

    HCV Antibiotic Infection
    Myriocin, a fungal metabolite isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin strongly suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
  • HY-14521
    Lometrexol

    DDATHF

    Antifolate Apoptosis Cancer
    Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
  • HY-100022
    Tomivosertib

    eFT508

    MNK PD-1/PD-L1 Cancer
    Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines. Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance.
  • HY-19269
    FK706

    Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect.
  • HY-14521B
    Lometrexol hydrate

    DDATHF hydrate

    Antifolate Apoptosis Cancer
    Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
  • HY-50751
    Linifanib

    ABT-869; AL-39324

    PDGFR VEGFR FLT3 c-Fms c-Kit Autophagy Apoptosis Cancer
    Linifanib (ABT-869) is a potent and orally active multi-target inhibitor of VEGFR and PDGFR family with IC50s of 4, 3, 66, and 4 nM for KDR, FLT1, PDGFRβ, and FLT3, respectively. Linifanib shows prominent antitumor activity. Linifanib has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib is a specific miR-10b inhibitor that blocks miR-10b biogenesis.
  • HY-125959
    Ucf-101

    Apoptosis Neurological Disease Cardiovascular Disease
    Ucf-101 is a selctive and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
  • HY-13775
    XL019

    JAK Apoptosis Cancer
    XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.