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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
28 Results for "
active site cysteine
" in MedChemExpress (MCE) Product Catalog:
Products (28)
28 Results for "active site cysteine" in MCE Product Catalog:
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6 Publications Verification
PACMA 31 is an irreversible, orally active protein disulfide isomerase (PDI) inhibitor with an IC50 of 10 μM. PACMA 31 forms a covalent bond with the active site cysteines of PDI. PACMA 31 shows tumor targeting ability and significantly suppresses ovarian tumor growth without causing toxicity to normal tissues . PACMA 31 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes.?I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST .
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3 Cited Publications
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
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2 Cited Publications
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MY-1B is a covalent inhibitor of the RNA Methyltransferase NSUN2 (IC50: 1.3 μM). MY-1B stereoselectively ligands active-site cysteine residues (C271) of NSUN2. MY-1B can stereoselectively and covalently bind to PSME1, disrupting the proteasome regulatory complex and downregulating the presentation of specific MHC-I subtypes .
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2 Cited Publications
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7-Azido-4-methylcoumarin is a selective coumarin-based fluorescent probe for hydrogen sulfide (H2S). In the presence of H2S, the aromatic azido group of 7-Azido-4-methylcoumarin is selectively reduced to produce the fluorescently active 7-amino-4-methylcoumarin (AMC). 7-Azido-4-methylcoumarin binds to the coumarin/phenol-binding site of BSA, the aglycone-binding site of UGT1A6, and the substrate-binding site of SULT1A1, respectively. 7-Azido-4-methylcoumarin retains its fluorescent properties after covalent binding, acts as a fluorescent H2S probe, and does not react with cysteine, homocysteine or glutathione (Ex/Em = 340/445 nm) .
Synonyms: BBSKE
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
Cat. No.: HY-171036
CAS No.: 252212-58-1
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GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC50 of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD +, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .
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8RK64 is a UCHL1 inhibitor that covalently binds the active-site cysteine residue to form an isothiourea adduct, with selectivity over UCHL3, UCHL5, and other cysteine DUBs. 8RK64 inhibits human UCHL1 with an IC50 of 0.32 μM. 8RK64 is an azide-containing precursor usable as a two-step activity-based probe via click chemistry. 8RK64 can be used for the research of Parkinson's disease .
Cat. No.: HY-12679
CAS No.: 1621002-24-1
PF-06658607 is an alkynylated irreversible Brutons tyrosine kinase (BTK) inhibitor that covalently reacts with active site cysteines in the ATP-binding pocket. PF-06658607 can be used to detect "off "-targets for covalent kinase inhibitors in cancer cells. The alkyne moiety allows for azide-based detection probe via copper-catalyzed click chemistry .
Cat. No.: HY-D2188
Cat. No.: HY-D2994
CAS No.: 2434651-49-5
Synonyms: SNAP-MaP555
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SPY555-BG (SNAP-MaP555) is a cell-permeable fluorescent dye for SNAP-tag labeling of HIV-1 Gag, which enables visualization of HIV-1 intercellular transmission via SNAPf. SPY555-BG relies on irreversible covalent binding to the active-site cysteine of the SNAPf tag fused to HIV-1 Gag .
Cat. No.: HY-W671129
CAS No.: 68930-68-7
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Cat. No.: HY-P10828
CAS No.: 1260620-30-1
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Cat. No.: HY-158378
CAS No.: 3058726-63-6
Synonyms: R-AST-OH
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Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
Cat. No.: HY-137028
CAS No.: 136904-69-3
Synonyms: PD157432
2'-Thioadenosine (PD157432) is a selective and irreversible inhibitor of ErbB-1 and ErbB-2, with an IC50 of 45 µM for ErbB-2. 2'-Thioadenosine covalently inactivates ErbB-1 via modification of a cysteine residue at the active site .
Cat. No.: HY-102087R
CAS No.: 262381-84-0
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JPM-OEt (Standard) is the analytical standard of JPM-OEt (HY-102087). This product is intended for research and analytical applications. JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
Cat. No.: HY-183387
CAS No.: 1348565-08-1
K11002 hydrobromide is a cysteine protease inhibitor. K11002 hydrobromide forms a covalent bond with the active site cysteine residue via Michael addition. K11002 hydrobromide inhibits the growth of Trypanosoma brucei. K11002 hydrobromide can be used in the research of African human trypanosomiasis (sleeping sickness) .
Cat. No.: HY-N11721
CAS No.: 138373-23-6
Cat. No.: HY-L925
9,363 compounds
Cysteine proteases (CPs), a key enzyme family regulating physiological metabolism and mediating pathological processes (such as abnormal bone resorption, tumour invasion, and pathogen infection), represent a core therapeutic target for developing specific inhibitors in disease intervention. Currently reported CP inhibitors primarily achieve their inhibitory function by precisely binding to CP active pockets (e.g., S1-S4 non-primed regions or S1'-S2' primed regions) and forming covalent/non-covalent interactions with the active site cysteine residues, providing clear structural references for the development of novel inhibitors.
This compound library, designed based on the core strategy of "similarity-based known active structures", contains over 200 cysteine protease inhibitors. Leveraging AI-driven molecular screening technology, it retains the critical pharmacological and shape features of reported CP inhibitors, serving as a specialized tool for efficiently discovering novel cysteine protease inhibitors.
Cat. No.: HY-183406
CAS No.: 102616-62-6
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AS15 is a PDIA1 inhibitor with an IC50 value of 300 nM. AS15 interacts with the active-site cysteine of PDIA1, and this process is independent of the substrate-binding domain of PDIA1. AS15 acts as a synergistic cell growth inhibitor with buthionine sulfoximine (BSO) (HY-106376), a glutathione synthesis inhibitor. AS15 can be used in the research of glioblastoma .
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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
