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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
35 Results for "
catalytic pocket
" in MedChemExpress (MCE) Product Catalog:
Products (35)
35 Results for "catalytic pocket" in MCE Product Catalog:
Target:
Research Areas:
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment .
PDK1-IN-RS2 is a mimic of peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor with a Kd of 9 μM. PDK1-IN-RS2 suppresses the activation of the downstream kinases S6K1 by PDK1 .
Cat. No.: HY-16138
CAS No.: 936221-33-9
Synonyms: CG-200745
Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects .
Cat. No.: HY-16138A
CAS No.: 3078712-42-9
Synonyms: CG-200745 formic
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Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat formic induces apoptosis and has anti-tumour effects .
Cat. No.: HY-174423
CAS No.: 1994348-72-9
Synonyms: NC-656
Iptriazopyrid is a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, with a Ki value of 24.3 nM against Arabidopsis thaliana and 33.3 nM against Oryza sativa. Iptriazopyrid binds to the active pocket of HPPD, occupies the catalytic site, inhibits carotenoid biosynthesis, prevents chloroplast formation, and induces albino and chlorotic symptoms in sensitive plants. Used as a herbicide, Iptriazopyrid can control barnyardgrass when applied alone, and its efficacy does not decrease when mixed with labeled residual herbicides. When Iptriazopyrid is mixed with 2,4-D or triclopyr, its barnyardgrass control effect shows an antagonistic effect. Iptriazopyrid is a triazole carboxamide herbicide that exhibits selectivity for Oryza sativa over Echinochloa crus-galli, and has partial tank-mix compatibility with synthetic auxin herbicides registered for rice .
Cat. No.: HY-P3818
CAS No.: 813416-46-5
Cat. No.: HY-126233
CAS No.: 1689554-51-5
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PAT-347 is an inhibitor of autotaxin (ATX, ENPP-2) . PAT-347 binds only to the hydrophobic channel of ATX, without occupying its hydrophobic pocket and catalytic site . PAT-347 blocks the binding of lysophosphatidylcholine (LPC) to the catalytic site of ATX .
Cat. No.: HY-168432
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KK181N1 is a potent inhibitor of karrikin (KAR) receptor KAI2. KK181N1 binds to the catalytic pockets of KAI2 in a non-covalent binding manner. KK181N1 selectively depress the KAR-induced phenotypes in Arabidopsis .
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α-Glucosidase-IN-22 (Compound 7i) is a α-glucosidase inhibitor with an IC50 value of 0.64 μM. α-Glucosidase-IN-22 can be used for the research of type 2 diabetes .
Cat. No.: HY-158038
CAS No.: 3035323-39-5
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AurkA allosteric-IN-1 (compound 6h) is an Aurora A (AurkA) inhibitor (IC50: 6.50 μM) that inhibits the catalytic activity and non-catalytic functions of Aurora A. Aurora A regulates the assembly of the bipolar mitotic spindle and the fidelity of chromosome segregation during mitosis and has non-catalytic functions. AurkA allosteric-IN-1 blocks the interaction of AurkA with the activator TPX2 by binding to the Y pocket of AurkA .
Cat. No.: HY-124308
CAS No.: 1221964-50-6
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
Cat. No.: HY-N12399
CAS No.: 3027425-38-0
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Cat. No.: HY-153802
CAS No.: 2841750-32-9
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Antitumor agent-100 is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 binds to the catalytic pocket of PDE3A, extends hydrophobic groups to mediate the hydrophobic interaction between PDE3A and SLFN12, and stabilizes the PDE3A-SLFN12 complex. Antitumor agent-100 induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 can be used for the research of cervical cancer .
Cat. No.: HY-153802A
CAS No.: 2841750-53-4
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Antitumor agent-100 hydrochloride is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 hydrochloride binds to the catalytic pocket of PDE3A, extends hydrophobic groups to mediate the hydrophobic interaction between PDE3A and SLFN12, and stabilizes the PDE3A-SLFN12 complex. Antitumor agent-100 hydrochloride induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 hydrochloride can be used for the research of cervical cancer .
Cat. No.: HY-126229
CAS No.: 1682644-84-3
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PAT-078 is a type II autotaxin (ATX) inhibitor. PAT-078 mainly occupies the hydrophobic pocket of ATX, blocks the bottleneck region between the hydrophobic channel and the catalytic site, and does not interact with the zinc ion at the catalytic site .
Cat. No.: HY-182615
CAS No.: 145209-39-8
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Cymserine is a blood-brain barrier-permeable butyrylcholinesterase (BuChE) inhibitor with an IC50 value of 56.43 nM and a Ki of 38 nM. Cymserine binds to the catalytic domain of BuChE in a concentration-dependent manner to form a stable carbamylated enzyme complex, and exhibits BuChE selectivity over acetylcholinesterase due to its structural compatibility with the larger acyl-binding pocket of BuChE. Cymserine can be used in the research of Alzheimer's disease .
Cat. No.: HY-187383
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Carbonic anhydrase-IN-40 is a human carbonic anhydrase I/II inhibitor, with an IC50 of 16.900 nM against hCA I and an IC50 of 4.682 nM against hCA II. Carbonic anhydrase-IN-40 binds to the active site of the enzyme, coordinates with the catalytic zinc ion, forms π-π stacking interactions with active site residues, and makes hydrophobic contacts with the hydrophobic pocket. Carbonic anhydrase-IN-40 can serve as a lead compound for studies related to carbonic anhydrase inhibitors .
Cat. No.: HY-181698
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MMP13-IN-6 (Compound 10a) is a MMP-13 inhibitor with a Ki value of 40 nM against hMMP-13. MMP13-IN-6 can be used in the research of osteoarthritis and rheumatoid arthritis .
Cat. No.: HY-183060
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Antitumor agent-215 is an antitumor agent. Antitumor agent-215 occupies the binding pocket of thymidylate synthase and interacts with key catalytic residues. Antitumor agent-215 induces cancer cell apoptosis and cell cycle arrest, and inhibits cell proliferation. Antitumor agent-215 can be used in the research of breast cancer and colorectal cancer .
Cat. No.: HY-137744
CAS No.: 148821-01-6
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MANT-GppNHp is a competitive adenyl cyclase (AC) inhibitor. MANT-GppNHp is a fluorescently labeled GTP (HY-113225) analogue. MANT-GppNHp interacts with the hydrophobic pocket near the AC catalytic site through its MANT group, thereby directly blocking the binding of the substrate ATP. MANT-GppNHp can be used to study diseases related to the increased activity of AC (such as cholera) .
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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
