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Targets Recommended: Ser/Thr Protease SRPK
Results for "

Serine endopeptidases

" in MCE Product Catalog:

160

Inhibitors & Agonists

3

Screening Libraries

1

Dye Reagents

1

Biochemical Assay Reagents

20

Peptides

2

MCE Kits

18

Natural
Products

119

Recombinant Proteins

17

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-113951
    Prolyl Endopeptidase Inhibitor 1

    Boc-Pro-prolinal; (Boc)-Prolyl-prolinal; BPP

    Dipeptidyl Peptidase Neurological Disease
    Prolyl Endopeptidase Inhibitor 1 (Boc-Pro-prolinal) is a potent prolyl endopeptidase (PEP; PE) inhibitor, with a Ki value of 15 nM. Prolyl Endopeptidase Inhibitor 1 has anti-amnesic effect.
  • 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-N0650S8
    L-Serine-d3

    (-)-Serine-d3; (S)-Serine-d3

    Endogenous Metabolite Cancer
    L-Serine-d3 ((-)-Serine-d3) is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S7
    L-Serine-d2

    (-)-Serine-d2; (S)-Serine-d2

    Endogenous Metabolite Cancer
    L-Serine-d2 ((-)-Serine-d2) is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S10
    L-Serine-15N

    (-)-Serine-15N; (S)-Serine-15N

    Endogenous Metabolite Cancer
    L-Serine-15N ((-)-Serine-15N) is the 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S1
    L-Serine-13C

    (-)-Serine-13C; (S)-Serine-13C

    Endogenous Metabolite Cancer
    L-Serine-13C ((-)-Serine-13C) is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S11
    L-Serine-d7

    (-)-Serine-d7; (S)-Serine-d7

    Endogenous Metabolite
    L-Serine-d7 is the deuterium labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S2
    L-Serine-1-13C

    (-)-Serine-1-13C; (S)-Serine-1-13C

    Endogenous Metabolite Cancer
    L-Serine-1-13C ((-)-Serine-1-13C) is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S4
    L-Serine-2-13C

    (-)-Serine-2-13C; (S)-Serine-2-13C

    Endogenous Metabolite Cancer
    L-Serine-2-13C ((-)-Serine-2-13C) is the 13C-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S
    L-Serine-13C3

    (-)-Serine-13C3; (S)-Serine-13C3

    Endogenous Metabolite Cancer
    L-Serine-13C3 ((-)-Serine-13C3) is the 13C-labeled L-Serine. 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-N0650S9
    L-Serine-15N,d3

    (-)-Serine-15N,d3; (S)-Serine-15N,d3

    Endogenous Metabolite Cancer
    L-Serine-15N,d3 ((-)-Serine-15N,d3) is the deuterium and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S6
    L-Serine1-13C,15N

    (-)-Serine-13C,15N; (S)-Serine-13C,15N

    Endogenous Metabolite Cancer
    L-Serine1-13C,15N ((-)-Serine-13C,15N) is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-N0650S5
    L-Serine-13C3,15N

    (-)-Serine-13C3,15N; (S)-Serine-13C3,15N

    Endogenous Metabolite Cancer
    L-Serine-13C3,15N ((-)-Serine-13C3,15N) is the 13C- and 15N-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • 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-N0650S3
    L-Serine-13C3,15N,d3

    (-)-Serine-13C3,15N,d3; (S)-Serine-13C3,15N,d3

    Endogenous Metabolite Cancer
    L-Serine-13C3,15N,d3 ((-)-Serine-13C3,15N,d3; (S)-Serine-13C3,15N,d3) is the deuterium, 13C-, and 15-labeled L-Serine. L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
  • HY-17399
    Racecadotril

    Acetorphan

    Neprilysin Metabolic Disease
    Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.
  • HY-100808
    D-Serine

    (R)-Serine

    iGluR Endogenous Metabolite Neurological Disease
    D-Serine ((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. D-Serinee 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-136276
    DMNB-caged-Serine

    Others Others
    DMNB-caged-Serine is a photocaged amino acid. DMNB is a caging group which is sensitive to blue light. DMNB-caged-Serine can be incorporated into proteins in Saccharomyces cerevisiae in response to the amber nonsense codon TAG, which can be helpful for controlling the chemical composition of mammalian proteins. .
  • HY-15129S
    O-Phospho-L-serine-13C3,15N

    L-Serine O-phosphate-13C3,15N; L-SOP-13C3,15N

    mGluR Endogenous Metabolite Neurological Disease
    O-Phospho-L-serine-13C3,15N (L-Serine O-phosphate-13C3,15N) is the 13C- and 15N-labeled O-Phospho-L-serine. 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[1].
  • 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-15114
    S 17092

    S 17092-1

    Others Neurological Disease
    S 17092 (S 17092-1) is a potent cerebral prolyl-endopeptidase (PEP) inhibitor with an IC50 of 1.2 nM. S 17092 can be used for the research of memory impairment and cognitive disorders associated with cerebral aging.
  • HY-139097
    C12-Sphingosine

    Others Others
    C12-Sphingosine is a short-chain Sphingosine homologue. C12-Sphingosine inhibits serine palmitoyltransferase activity in primary cultured cerebellar cells.
  • HY-141613
    1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium

    Others Others
    1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium is a ubstitute for Phosphoserine/phosphatidylserine. 1,2-Dioleoyl-sn-glycero-3-phospho-L-serine sodium can be used in lipid mixtures with DOPC and DOPE as effective nontoxic and nonviral DNA vectors.
  • HY-119759
    Lipoxamycin

    Fungal Infection
    Lipoxamycin is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • 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-119759A
    Lipoxamycin hemisulfate

    Fungal Infection
    Lipoxamycin hemisulfate is an antifungal antibiotic and a potent serine palmitoyltransferase inhibitor with an IC50 of 21 nM.
  • HY-P3101
    GLP-1(28-36)amide

    Glucagon Receptor Metabolic Disease Cardiovascular Disease
    GLP-1(28-36)amide, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide has anti-diabetic and cardioprotection effects.
  • 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-18544
    AA38-3

    MAGL FAAH Metabolic Disease
    AA38-3 is a serine hydrolase (SH) inhibitor. AA38-3 can inhibit three SHs, ABHD6, ABHD11, and FAAH.
  • HY-P3101A
    GLP-1(28-36)amide TFA

    Glucagon Receptor Metabolic Disease Cardiovascular Disease
    GLP-1(28-36)amide TFA, a C-terminal nonapeptide of GLP-1, is a major product derived from the cleavage of GLP-1 by the neutral endopeptidase (NEP). GLP-1(28-36)amide TFA is an antioxidant and targets to mitochondrion, inhibits mitochondrial permeability transition (MPT). GLP-1(28-36)amide TFA has anti-diabetic and cardioprotection effects.
  • 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 endocannabinoid-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-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-W174279
    Tyrphostin 8

    EGFR Ras Phosphatase Metabolic Disease
    Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM).
  • HY-145263
    VD2173

    Ser/Thr Protease Cancer
    VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer.
  • HY-19649
    Candoxatril

    UK 79300

    Neprilysin Metabolic Disease
    Candoxatril is a neutral endopeptidase (NEP) inhibitor.
  • HY-101962
    HNMPA

    Insulin Receptor Metabolic Disease
    HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
  • HY-136069
    Xeruborbactam

    QPX7728

    Bacterial Infection
    Xeruborbactam (QPX7728) is a potent, ultra-broad-spectrum boronic acid beta-lactamase inhibitor. Xeruborbactam inhibits key serine and metallo beta-lactamases at a nano molar range.
  • 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-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-U00294
    NEP-In-1

    Neprilysin Neurological Disease
    NEP-IN-1 is a neutral endopeptidase (NEP) inhibitor with IC50 of 2 nM for dNEP.
  • HY-145860
    PHGDH-IN-2

    Others Cancer
    PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells.
  • HY-120129
    Ancremonam

    BOS-228; LYS-228

    Bacterial Infection
    Ancremonam (LYS-228) is a low toxicity, potent and single-agent monobactam antibiotic targeting penicillin binding protein 3 with potent activity against Enterobacteriaceae. Ancremonam kills bacteria by inhibiting cell wall synthesis through covalent modification of the active-site serine of penicillin binding protein 3.
  • HY-125351
    SPT-IN-1

    Others Metabolic Disease
    SPT-IN-1 (compound 1) is an orally active and potent SPT (serine palmitoyl transferase) inhibitor, with an IC50 of 5.19 nM for hSPT1. SPT-IN-1 can be used for type 2 diabetes and dyslipidemia research.
  • HY-N6902
    Linderene acetate

    Others Inflammation/Immunology
    Linderene acetate, isolated from the root of Lindera strychnifolia, is a prolyl endopeptidase inhibitor.
  • HY-U00336
    NEP-IN-2

    Neprilysin Cardiovascular Disease
    NEP-IN-2 is an inhibitor of neutral endopeptidase, used in the research of proliferation in atherosclerosis, restenosis.
  • HY-137458
    Vevorisertib

    ARQ 751

    Akt Cancer
    Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations.
  • HY-124379
    TPCK

    L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK

    Ser/Thr Protease Cancer Inflammation/Immunology
    TPCK (L-1-Tosylamido-2-phenylethyl chloromethyl ketone; L-TPCK) is a potent serine protease inhibitor that reacts with the retinoblastoma protein (RB)-binding core of HPV-18 E7 protein and abolish its RB-binding capability. TPCK is able to modify E7 protein in live keratinocytes following its addition to the culture medium.
  • HY-107761
    JMV 390-1

    Others Neurological Disease
    JMV 390-1 (Compound 6a) is a potent multipeptidase inhibitor. JMV 390-1 behaves as a full inhibitor of the major neurotensin (NT)/neuromedin N (NN) degrading enzymes in vitro with IC50 values from 30 to 60 nM. JMV 390-1 increases endogenous recovery of NT and NN from slices of mice hypothalamus depolarized with potassium.
  • HY-P1484
    Bradykinin (1-7)

    Bradykinin Fragment 1-​7

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (1-7) is an amino-truncated Bradykinin peptide. Bradykinin (1-7) is a metabolite of Bradykinin, cleaved by endopeptidase.
  • HY-143868
    HPK1-IN-27

    MAP4K Cancer
    HPK1-IN-27 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-27 has the potential for the research of cancer diseases (extracted from patent WO2019016071A1, compound 38).
  • HY-143871
    HPK1-IN-30

    MAP4K Cancer
    HPK1-IN-30 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-30 has the potential for the research of cancer diseases (extracted from patent WO2021175271A1, compound 3).
  • 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-P1497
    Bradykinin (1-3)

    Bradykinin Receptor Cardiovascular Disease Endocrinology
    Bradykinin (1-3) is a 3-amino acid residue peptide. Bradykinin (1-3) is an amino-truncated Bradykinin peptide, cleaved by Prolyl endopeptidase.
  • HY-U00171
    SQ28603

    SQ28,603; Squibb 28603

    Neprilysin Metabolic Disease
    SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
  • HY-P2329
    Lysostaphin

    Bacterial Antibiotic Infection Inflammation/Immunology
    Lysostaphin is an antistaphylococcal agent. Lysostaphin has activities of three enzymes namely, glycylglycine endopeptidase, endo-β-N-acetyl glucosamidase and N-acteyl muramyl-L-alanine amidase.
  • HY-N2021A
    Phosphoramidon Disodium

    Angiotensin-converting Enzyme (ACE) Neprilysin Inflammation/Immunology Cardiovascular Disease Cancer
    Phosphoramidon Disodium is a metalloprotease inhibitor. Phosphoramidon inhibits endothelin-converting enzyme (ECE), neutral endopeptidase (NEP), and angiotensin-converting enzyme (ACE) with IC50 values of 3.5, 0.034, and 78 μM, respectively.
  • HY-N0109
    Salidroside

    Rhodioloside

    mTOR Apoptosis Cancer
    Salidroside is a prolyl endopeptidase inhibitor. Salidroside alleviates cachexia symptoms in mouse models of cancer cachexia via activating mTOR signalling. Salidroside protects dopaminergic neurons by enhancing PINK1/Parkin-mediated mitophagy.
  • HY-B0385
    Gabexate mesylate

    FOY

    Factor Xa Proteasome Inflammation/Immunology
    Gabexate mesylate is a Factor X inhibitor; serine protease inhibitor .
  • 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-112205A
    RR-11a analog

    Parasite Infection
    RR-11a analog is a potent and selective inhibitors of asparaginyl endopeptidases (AE) (Legumain), with IC50 values of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.
  • HY-12821
    AEBSF hydrochloride

    Thrombin Influenza Virus Ser/Thr Protease Others
    AEBSF hydrochloride is an irreversible inhibitor of serine proteases, such as chymotrypsin, kallikrein, plasmin, thrombin, and trypsin.
  • HY-N9725
    16-Hydroxycleroda-3,13-dien-15,16-olide

    16ξ-Hydroxycleroda-3,13-dien-15,16-olide

    Dipeptidyl Peptidase Metabolic Disease
    16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy.
  • HY-114174
    Fmoc-Ala-Glu-Asn-Lys-NH2

    Amyloid-β Neurological Disease
    Fmoc-Ala-Glu-Asn-Lys-NH2 is a selective asparagine endopeptidase (AEP) inhibitor peptide and suppresses amyloid precursor protein (APP) cleavage. AEP, a pH-controlled cysteine proteinase, is activated during ageing and mediates APP proteolytic processing.
  • 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-107582
    JW480

    Others Cancer
    JW480 is a potent and selective inhibitor of a serine hydrolase enzyme KIAA1363.
  • HY-137456
    Tilpisertib

    GS-4875

    Ser/Thr Protease Cancer Inflammation/Immunology
    Tilpisertib (GS-4875) is a serine/threonine kinase inhibitor (WO2017007689).
  • HY-N2454
    β-Elemonic acid

    Apoptosis Reactive Oxygen Species COX Cancer Inflammation/Immunology
    β-Elemonic acid is a triterpene isolated from Boswellia papyrifera. β-Elemonic acid induces cell apoptosis, reactive oxygen species (ROS) and COX-2 expression and inhibits prolyl endopeptidase. β-Elemonic acid exhibits anticancer and anti-inflammatory effects.
  • 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-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-17399S
    Racecadotril-d5

    Acetorphan-d5

    Neprilysin Metabolic Disease
    Racecadotril-d5 (Acetorphan-d5) is the deuterium labeled Racecadotril. Racecadotril (Acetorphan) is a neutral endopeptidase (NEP) inhibitor. Racecadotril and its active metabolite Thiorphan inhibits purified NEP activity from mouse brain with Kis of 4500 and 6.1 nM, , respectively. Antidiarrheal agent.
  • HY-145349
    FXIa-IN-6

    Factor Xa Cardiovascular Disease
    FXIa-IN-6 is a potent FXIa inhibitor with selectivity against most of the relevant serine proteases (Ki = 0.3 nM).
  • HY-139568
    Deutarserine

    CTP-692

    Endogenous Metabolite Neurological Disease
    Deutarserine is a deuterium modified analog of endogenous D-serine (CTP 692), which is used in the research of adults with schizophrenia.
  • 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-135893
    SGK1-IN-2

    SGK Inflammation/Immunology
    SGK1-IN-2 (14h) is a selective SGK1 (serum and glucocorticoid regulated kinase 1) inhibitor, with an IC50 of 5 nM at 10 μM ATP concentration.
  • 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-101682
    SCH 42495

    Neprilysin Cardiovascular Disease
    SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • HY-101682A
    SCH 42495 racemate

    Neprilysin Cardiovascular Disease
    SCH 42495 racemate is the racemate of SCH 42495. SCH 42495 is an orally active neutral metalloendopeptidase (NEP) inhibitor with antihypertensive effect. SCH 42495 is the orally active ethylester prodrug of SCH 42354.
  • 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-147519
    ARUK3001185

    Wnt Cancer
    ARUK3001185 (Compound 8l) is a potent, selective, orally active and brain-penetrant inhibitor of Notum activity with an IC50 of 6.7 nM.
  • HY-123348
    Sampatrilat

    UK-81252

    Angiotensin-converting Enzyme (ACE) Neprilysin Inflammation/Immunology Cardiovascular Disease
    Sampatrilat (UK-81252) is a potent and orally active vasopeptidase inhibitor of ACE and neutral endopeptidase (NEP). Sampatrilat inhibits C-domain ACE (Ki=13.8 nM) 12.4-fold more potent than that for the N-domain (Ki=171.9 nM). Sampatrilat (UK-81252) can be used for the study of chronic heart failure and blood pressure regulation.
  • 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-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-114164
    Thrombin (MW 37kDa)

    Thrombin Neurological Disease
    Thrombin (MW 37kDa) is a Na +-activated, allosteric serine protease that plays opposing functional roles in blood coagulation. Thrombin recognition sequence and can be used to digest GST-tagged 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-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-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-111866
    PROTAC RIPK degrader-2

    PROTACs RIP kinase Inflammation/Immunology
    PROTAC RIPK degrader-2 is a nonpeptidic PROTAC based on von Hippel-Lindau ligand which potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.
  • 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 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-P3150
    Recombinant Proteinase K

    Ser/Thr Protease Others
    Recombinant Proteinase K is a serine protease that cleaves the carboxy-terminated peptide bonds of aliphatic and aromatic amino acids. Recombinant Proteinase K can be used to digest proteins and remove contamination from nucleic acid preparations.
  • 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-144088
    ZYF0033

    HPK1-IN-22

    MAP4K Cancer Inflammation/Immunology
    ZYF0033 (HPK1-IN-22, compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 decreases the phosphorylation of SLP76 (serine 376). ZYF0033 promotes anticancer immune responses. ZYF0033 inhibits tumor growth and caused increases intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells but decreased infiltration of regulatory T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells in the 4T-1 syngeneic mouse model.
  • 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-126361
    ZK824190

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • HY-126361A
    ZK824190 hydrochloride

    Ser/Thr Protease PAI-1 Inflammation/Immunology
    ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  • 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-14853
    Darexaban

    YM150

    Factor Xa Ser/Thr Protease Cardiovascular Disease
    Darexaban (YM150) is a potent, selective and orally active factor Xa (FXa) inhibitor with an IC50 of 54.6 nM. Darexaban shows high selectivity against other related serine proteases, such as trypsin, thrombin, and kallikrein. Darexaban has anticoagulant and antithrombotic effects.
  • 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-N10223
    Phostriecin

    Antibiotic Phosphatase Cancer Infection Inflammation/Immunology
    Phostriecin is an antitumor antibiotic produced by Streptomyces pulveraceus. Phostriecin is a strong inhibitor of type 2A (PP2A) and a weak inhibitor of type 1 (PP1) serine/threonine protein phosphatases with IC50s of 3.2 nM and 131 μM, respectively. Phostriecin has the potential for the research of cancer.
  • 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-130517
    Cdc7-IN-5

    CDK Cancer
    Cdc7-IN-5 (compound I-B) 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-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-132605
    SLN124

    Ser/Thr Protease Metabolic Disease
    SLN124 is a GalNac-siRNA targeting transmembrane serine protease 6 (Tmprss6). SLN124 is composed of a trimeric GalNAc ligand conjugated to TMPRSS6‐siRNA. SLN124 has the potential for an siRNA to restore hepcidin expression and normalise iron homeostasis in β‐thalassaemia.
  • 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 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-10300
    Narlaprevir

    SCH 900518

    HCV HCV Protease SARS-CoV 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 also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 2.3 μM.
  • HY-142686
    SGK1-IN-3

    SGK Inflammation/Immunology
    SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis.
  • HY-103645
    GW779439X

    Bacterial Aurora Kinase Apoptosis Cancer Infection
    GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
  • HY-139744
    FPI-1465

    Bacterial Infection
    FPI-1465 acts a dual inhibitor of serine-β-Lactamases and Penicillin-binding proteins (PBPs).FPI-1465 inhibits PBP2 (IC50=1.0 µg/mL). FPI-1465 exhibits activity against β-lactamase CTX-M-15 and OXA-48 with Kds of 0.011 and 5.3 µM, respectively.
  • HY-143377
    Cdc7-IN-8

    CDK Cancer
    Cdc7-IN-8 is a potent inhibitor of Cdc7. Cdc7 is a serine/threonine kinase which activates MCM promotion by phosphorylating the microchromosome maintenance protein (MCM protein), an important element of the DNA replication initiator. Cdc7-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021032170A1, compound 1-1/1-2).
  • HY-114015
    APC-6860

    Ser/Thr Protease Cancer
    APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21 and 0.44 μM for uPA and trypsin, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.
  • HY-139439
    SBI-581

    Others Cancer
    SBI-581 is an orally active and potent selective serine-threonine kinase TAO3 inhibitor, with an IC50 of 42 nM. SBI-581 promotes TKS5α accumulation at RAB11-positive vesicles. SBI-581 inhibits invadopodia formation. SBI-581 shows reasonable pharmacokinetics in mice using IP injection. SBI-581 shows antitumor activity.
  • HY-128035
    ML-211

    Phospholipase MAGL
    ML-211 is a carbamate-based dual inhibitor of acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) (IC50=17 nM) and LYPLA2 (IC50=30 nM). ML-211 also inhibits theserine hydrolase ABHD11 with an IC50 value of 10 nM but is ≥ 50-fold selective for LYPLA in a panel of 20 additional serine hydrolases.
  • 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-145039
    HPK1-IN-13

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-13 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) .
  • HY-145038
    HPK1-IN-12

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-12 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-12 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 85) .
  • HY-W181102
    NFAT Inhibitor-2

    Others Inflammation/Immunology Neurological Disease Cardiovascular Disease
    NFAT Inhibitor-2 is a potent inhibitor of calcineurin NFAT signalling. Calcineurin is a serine/threonine protein phosphatase regulated by Ca2+ and calmodulin. NFAT Inhibitor-2 has the potential for the research of inflammatory disease, an autoimmune disorder, a cardiovascular disease, a neurodegenerative disease, a disease occurring with uncontrolled cell proliferation and/or differentiation, an angiogenesis-related disease, an allergy, anaphylaxis and alopecia (extracted from patent WO2016207212A1, compound 17).
  • 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-145040
    HPK1-IN-14

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-14 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-14 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 79) .
  • 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-145035
    HPK1-IN-9

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) .
  • HY-145037
    HPK1-IN-11

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-11 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-11 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 2).
  • HY-145036
    HPK1-IN-10

    MAP4K Cancer Inflammation/Immunology
    HPK1-IN-10 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-10 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 103) .
  • 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-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-146581
    Cathepsin C-IN-4

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively.
  • HY-146580
    Cathepsin C-IN-3

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively.
  • HY-146584
    Cathepsin C-IN-5

    Cathepsin Inflammation/Immunology
    Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity.
  • HY-125959
    Ucf-101

    Apoptosis Neurological Disease Cardiovascular Disease
    Ucf-101 is a selective 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.