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effective substrate

" in MedChemExpress (MCE) Product Catalog:

12

Inhibitors & Agonists

2

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100875
    Bisantrene
    5 Publications Verification

    CL216942

    		 Topoisomerase Cancer
    Bisantrene is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene targets eukaryotic type II topoisomerases. Bisantrene is a substrate of MDR1 .
    Bisantrene
  • HY-100875A
    Bisantrene dihydrochloride
    5 Publications Verification

    CL-216942 dihydrochloride

    		 Topoisomerase Cancer
    Bisantrene dihydrochloride is a highly effective antitumor agent, it exerts its cytotoxicity by affecting DNA intercalation. Bisantrene dihydrochloride targets eukaryotic type II topoisomerases. Bisantrene dihydrochloride is a substrate of MDR1 .
    Bisantrene dihydrochloride
  • HY-164495
    Sob-AM2

    		FAAH Thyroid Hormone Receptor Inflammation/Immunology Endocrinology
    Sob-AM2 is a potent substrate (Km=1.3 μM) targeting fatty acid amide hydrolase (FAAH) expressed in the brain and has blood-brain barrier permeability. Sob-AM2 delivers high concentrations of Sobetirome (HY-14823) to the central nervous system with minimal peripheral systemic dose, thereby stimulating central thyroid hormone receptor β (TRβ). In addition, Sob-AM2 can prevent myelin and axon degeneration in experimental autoimmune encephalomyelitis (EAE) mice .
    Sob-AM2
  • HY-108544
    INCA-6
    1 Publications Verification

    Triptycene-1,4-quinone

    		 Nuclear Factor of activated T Cells (NFAT) Cardiovascular Disease
    INCA-6 (Triptycene-1,4-quinone) is a cell-permeable NFAT inhibitor. INCA-6 specifically blocks targeting of NFAT(P) substrate to the ?calcineurin (CN) phosphatase site and is an effective inhibitor of CN-NFAT signaling .
    INCA-6
  • HY-111338
    Tacrine
    5 Publications Verification

    		 Cholinesterase (ChE) Neurological Disease
    Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
    Tacrine
  • HY-P2802
    α-Glucosidase, Yeast

    α-D-Glucosidase, Yeast

    		 Glucosidase Metabolic Disease
    α-Glucosidase, Yeast (α-D-Glucosidase, Yeast), a carbohydrate hydrolyzing enzyme, catalyzes the liberation of α-glucose from the non-reducing end of the substrate. α-Glucosidase can facilitate the absorption of glucose by the small intestine. Inhibition of α-Glucosidase is an effective management of non-insulin-dependent diabetes mellitus (NIDDM) .
    α-Glucosidase, Yeast
  • HY-P1906
    [pThr3]-CDK5 Substrate

    		CDK Neurological Disease
    [pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
    [pThr3]-CDK5 Substrate
  • HY-P1906A
    [pThr3]-CDK5 Substrate TFA

    		CDK Neurological Disease
    [pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
    [pThr3]-CDK5 Substrate TFA
  • HY-162654
    FXIIIa-IN-1

    		Others Cardiovascular Disease
    FXIIIa-IN-1 (Compound 16) is a potent and selective FXIIIa (Factor XIIIa) inhibitor with an IC50 value of 2.4 μM. FXIIIa-IN-1 inhibits FXIIIa by competing with the Gln-donor protein substrate (dimethylcasein). FXIIIa-IN-1 holds promise for the development of effective and safe novel anticoagulants .
    FXIIIa-IN-1
  • HY-117747
    DMP 323

    JCR 424; XM 323

    		 HIV Protease Infection
    DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
    DMP 323
  • HY-110137A
    Furamidine

    DB75; NSC 305831

    		 Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
    Furamidine
  • HY-110137
    Furamidine dihydrochloride
    2 Publications Verification

    DB75 dihydrochloride; NSC 305831 dihydrochloride

    		 Histone Methyltransferase Phosphodiesterase (PDE) Parasite Infection Inflammation/Immunology Cancer
    Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
    Furamidine dihydrochloride

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