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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
26 Results for "
effective substrate
" in MedChemExpress (MCE) Product Catalog:
Products (26)
26 Results for "effective substrate" in MCE Product Catalog:
51
51 Publications Verification
Cat. No.: HY-B0445A
CAS No.: 20111-18-6
Synonyms: β-DPN sodium; β-NAD sodium; β-Nicotinamide Adenine Dinucleotide sodium
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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 .
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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 .
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6 Cited Publications
Synonyms: CL-216942 dihydrochloride
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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 .
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4 Cited Publications
Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride
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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 .
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4 Cited Publications
Synonyms: Triptycene-1,4-quinone
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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 .
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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) .
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Cat. No.: HY-W406070
CAS No.: 207131-16-6
Synonyms: LNA-G
Research Areas:
2′-O,4′-C-Methyleneguanosine (LNA-G) is a reverse guanine analog, where LNA (locked nucleic acid) is a nucleic acid analog. LNA modification can be widely used in various fields, such as effective binding affinity with complementary sequences and stronger nuclease resistance than natural nucleotides, providing great potential for application in disease diagnosis and research. 2'-O,4'-C-Methyleneguanosine is a substrate for KOD DNA polymerase, which incorporates LNA-G nucleotides into growing DNA strands, including consecutive incorporations , to generate full-length extension products .
Cat. No.: HY-164495
CAS No.: 2128258-47-7
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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 .
Cat. No.: HY-110137A
CAS No.: 73819-26-8
Synonyms: DB75; NSC 305831
Research Areas:
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 .
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S-Adenosyl-L-ethionine is S-Adenosyl-L-methione analog. S-Adenosyl-L-ethionine is able to replace S-Adenosyl-L-methione during HydG catalysis. HydG can utilize S-Adenosyl-L-ethionine as an effective alternative cosubstrate to S-Adenosyl-L-methione under normal enzymatic turnover conditions, producing the Ω intermediate and allowing efficient catalytic turnover of substrate L-tyrosine .
Cat. No.: HY-160431
CAS No.: 82864-43-5
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8(9)-EET is one of the main metabolites produced by the metabolism of arachidonic acid (HY-109590) through the cytochrome P450 epoxide pathway. 8(9)-EET is an effective substrate for COX-1 and COX-2. 8(9)-EET activates PPARα in HEK293 cells and inhibits the activity of NF-κB induced by IL-1β in a PPARα-dependent and -independent manner. The (8S,9R)-isomer of 8(9)-EET ([(8S,9R)-EET]) causes vasoconstriction, thereby reducing renal plasma flow and glomerular filtration rate .
Cat. No.: HY-P1906
CAS No.: 1670273-47-8
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Cat. No.: HY-117747
CAS No.: 151867-81-1
Synonyms: JCR 424; XM 323
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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 .
Cat. No.: HY-153321A
CAS No.: 2649400-33-7
Synonyms: (R,R)-NX-5948; (R,R)-BTK-IN-24
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(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
Cat. No.: HY-P1906A
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Cat. No.: HY-100875R
CAS No.: 78186-34-2
Synonyms: CL216942 (Standard)
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Bisantrene (Standard) is the analytical standard of Bisantrene. This product is intended for research and analytical applications. 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 .
Cat. No.: HY-162654
CAS No.: 55909-92-7
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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 .
Cat. No.: HY-111338R
CAS No.: 321-64-2
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Tacrine (Standard) is the analytical standard of Tacrine. This product is intended for research and analytical applications. 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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
