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Targets Recommended: Nucleoside Antimetabolite/Analog

Results for "Antimetabolite Inhibitors" in MCE Product Catalog:

39

Inhibitors & Agonists

1

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-B0077
    Bendamustine hydrochloride

    SDX-105

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Bendamustine hydrochloride (SDX-105), a purine analogue, is a DNA cross-linking agent. Bendamustine hydrochloride activats DNA-damage stress response and apoptosis. Bendamustine hydrochloride has potent alkylating, anticancer and antimetabolite properties.
  • HY-13567
    Bendamustine

    SDX-105 free base

    DNA Alkylator/Crosslinker Apoptosis Cancer
    Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activats DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-130812
    Gemcitabine-O-Si(di-iso)-O-Mc

    Drug-Linker Conjugates for ADC Cancer
    Gemcitabine-O-Si(di-iso)-O-Mc is a drug-linker conjugate for ADC with potent antitumor activity by using Gemcitabine (a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent; HY-17026), linked via the ADC linker.
  • HY-106014
    Tezacitabine

    DNA/RNA Synthesis Nucleoside Antimetabolite/Analog Apoptosis Cancer
    Tezacitabine is a cytostatic and cytotoxic antimetabolite and a nucleoside analogue. Tezacitabine irreversibly inhibits the ribonucleotide reductase and interferes with DNA replication and repair. Tezacitabine effectively induces cells apoptotic. Tezacitabine has the potential for leukemias and solid tumors (carcinomas) treatment.
  • HY-123032
    Sorivudine

    BV-araU

    DNA/RNA Synthesis Infection
    Sorivudine (BV-araU) is an orally active synthetic pyrimidine nucleoside antimetabolite drug. Sorivudine derives its antiviral activity from selective conversion by a specific thymidine kinase present in certain DNA viruses to nucleotides, which can in turn interfere with viral DNA synthesis.
  • HY-B0097
    Floxuridine

    5-Fluorouracil 2'-deoxyriboside

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Bacterial CMV HSV Cancer Infection
    Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV.
  • HY-16200
    Ethynylcytidine

    ECyD; TAS-106; 3'-C-Ethynylcytidine

    Nucleoside Antimetabolite/Analog Cancer
    Ethynylcytidine is a new nucleoside antimetabolite.
  • HY-10821
    Raltitrexed

    ZD1694; D1694; ICI-D1694

    Thymidylate Synthase Nucleoside Antimetabolite/Analog Cancer
    Raltitrexed is an antimetabolite drug used in chemotherapy, acting by inhibiting thymidylate synthase.
  • HY-B0182
    Carmofur

    HCFU

    Nucleoside Antimetabolite/Analog Cancer
    Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent.
  • HY-107430
    Oxythiamine

    Hydroxythiamin

    Others Cancer
    Oxythiamine, an antimetabolite and a vitamin B1 antagonist, is a well-known thiamine antagonist and inhibitor of transketolase.
  • HY-121295
    Roseoflavin

    Bacterial Infection
    Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.
  • HY-B0069
    Fludarabine

    F-ara-A; NSC 118218

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT Apoptosis Cancer
    Fludarabine (NSC 118218) is a DNA synthesis inhibitor, which also inhibits phosphorylation of STAT1. Fludarabine, a pro-drug, is converted metabolically by dephosphorylation to the antimetabolite, F-ara-A.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-13538
    Gemcitabine (elaidate)

    CP-4126; CO-101; Gemcitabine 5'-elaidate

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Cancer
    Gemcitabine elaidate(CP-4126; CO-101) is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with potential antineoplastic activity.
  • HY-112732B
    Sparfosic acid trisodium

    Others Cancer Metabolic Disease
    Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis.
  • HY-13567S
    Bendamustine D4

    SDX-105 D4 free base

    DNA Alkylator/Crosslinker Cancer
    Bendamustine D4 (SDX-105 D4 free base) is the deuterium labeled Bendamustine. Bendamustine is a DNA cross-linking agent that causes DNA breaks, with alkylating and antimetabolite properties.
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-107093
    MBC-11

    Others Cancer
    MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research.
  • HY-107093B
    MBC-11 triethylamine

    Others Cancer
    MBC-11 triethylamine is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 triethylamine has the potential for tumor-induced bone disease (TIBD) research.
  • HY-107093A
    MBC-11 trisodium

    Others Cancer
    MBC-11 trisodium is a first-in-class conjugate of the bone-targeting bisphosphonate HEDP covalently linked to the antimetabolite Ara-C. MBC-11 trisodium has the potential for tumor-induced bone disease (TIBD) research.
  • HY-19373
    RWJ-445167

    3DP-10017

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

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-14519
    Methotrexate

    Amethopterin; CL14377; WR19039

    Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Cancer Inflammation/Immunology
    Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
  • HY-128671
    6-​Thioinosine

    6TI; 6-Mercaptopurine riboside

    Nucleoside Antimetabolite/Analog Metabolic Disease
    6-​Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent, downregulates mRNA levels of PPAR γ and C/EBPα, as well as PPAR γ target protein such as LPL, CD36, aP2, and LXRα.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

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

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-14519A
    Methotrexate disodium

    Amethopterin disodium; CL14377 disodium; WR19039 disodium

    Antifolate DNA/RNA Synthesis ADC Cytotoxin Apoptosis Cancer Inflammation/Immunology
    Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia).
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-A0004
    Decitabine

    5-Aza-2'-deoxycytidine; NSC 127716

    DNA Methyltransferase Apoptosis Nucleoside Antimetabolite/Analog Cancer
    Decitabine (NSC 127716) is a deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. Decitabine has potent anticancer activity.
  • HY-135813
    LtaS-IN-1

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

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

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

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-17026
    Gemcitabine

    LY 188011

    Nucleoside Antimetabolite/Analog DNA/RNA Synthesis Autophagy Apoptosis Cancer
    Gemcitabine (LY 188011) is a pyrimidine nucleoside analog antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis. Gemcitabine inhibits the growth of BxPC-3, Mia Paca-2, PANC-1, PL-45 and AsPC-1 cells with IC50s of 37.6 nM, 42.9 nM, 92.7 nM, 89.3 nM and 131.4 nM, respectively.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-122872
    MKK7-COV-9

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

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