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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
81 Results for "
hydrophobic pocket
" in MedChemExpress (MCE) Product Catalog:
Products (81)
81 Results for "hydrophobic pocket" in MCE Product Catalog:
3
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CPA inhibitor (Compound 5) (Carboxypeptidase inhibitor) is an orally active competitive carboxypeptidase A (CPA) inhibitor with a Ki value of 0.32 μM. CPA inhibitor blocks the activity of carboxypeptidase A3 (CPA3). CPA activator activates the Wnt/Lrp6/β-catenin signaling pathway. CPA inhibitor reduces epithelial damage. CPA inhibitor is applicable to research related to inflammatory bowel disease, including ulcerative colitis and Crohn's disease .
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Sebetralstat (KVD900) is an orally active and selective plasma kallikrein inhibitor, with an IC50 of 6.0 nM and a Ki of 3.0 nM against the human target. Sebetralstat binds to the active site of plasma kallikrein, inducing a conformational flip of Trp215 to form a U-shaped conformation; its P1 group interacts with the S1 pocket through hydrophobic interactions and displacement of high-energy water molecules, independent of the Asp189 ionic bond. Sebetralstat inhibits plasma kallikrein-kinin system activation in whole plasma, rapidly relieves laryngeal and abdominal attack symptoms of hereditary angioedema (HAE-C1INH), and reduces attack severity. Sebetralstat can be used in research related to hereditary angioedema (HAE) .
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Synonyms: MK-8507
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Ulonivirine is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor that binds to the classical non-nucleoside reverse transcriptase inhibitor hydrophobic binding pocket adjacent to the polymerase active site of HIV-1 reverse transcriptase. Ulonivirine can be used in studies related to HIV-1 infection .
Cat. No.: HY-W009123
CAS No.: 112-84-5
Synonyms: cis-13-Docosenamide
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Erucamide is an orally active, blood-brain barrier-permeable TMEM19 ligand and T3SS inhibitor. Erucamide exerts retinal neuroprotective effects in mouse models of retinal degeneration. Erucamide attenuates depression- and anxiety-like behaviors in mice.\n\nErucamide binds to the conserved hydrophobic pocket in HrcC, disrupts its outer membrane localization, and blocks T3SS-mediated effector protein secretion in Gram-negative pathogenic bacteria. Erucamide enhances the antimicrobial immunity of plants against pathogenic bacteria. Erucamide can be used in research related to retinitis pigmentosa, anxiety and depression, bacterial wilt, and bacterial blight .
Synonyms: ZM-H1505R
Canocapavir (ZM-H1505R) is an orally active HBV core protein-targeting antiviral agent. Canocapavir binds to the hydrophobic pocket at the dimer-dimer interface of HBV core protein (HBc), stimulating intracellular accumulation of nonfunctional HBV capsids, disrupting viral replication. Canocapavir interferes with the interaction between HBc and HBV large surface protein, resulting in diminished
production of empty virionsis. Canocapavir can be used for the research of hepatitis B virus (HBV) infection .
production of empty virionsis. Canocapavir can be used for the research of hepatitis B virus (HBV) infection .
Cat. No.: HY-D0074
CAS No.: 70504-01-7
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Prodan is an environment-sensitive fluorescent probe used to investigate the polarity, fluidity, and structure of lipid membranes. Prodan exhibits environment-dependent excitation/emission wavelengths, with its wavelength range covering Ex = 360-410 nm and Em = 430-530 nm when in solvents, bound to DNA, located in lipid bilayers, or associated with proteins. Prodan can interact with the major groove of DNA, regions of lipid bilayers, and hydrophobic pockets of proteins. During phase transitions, Prodan localizes to different regions of the bilayer: the emission minimum is 430-440 nm in the gel phase, while it shifts to 480-500 nm in the liquid-crystalline phase or interdigitated gel phase. When bound to rigid hydrophobic sites of proteins, the emission peak of Prodan undergoes a blue shift and its fluorescence intensity increases .
Cat. No.: HY-W014223
CAS No.: 131-56-6
Synonyms: Ultraviolet absorber UV-0
Target:
Environmental Pollutants Toll-like Receptor (TLR) NF-κB Reactive Oxygen Species (ROS) MyD88 IRAK
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2,4′-Dihydroxybenzophenone (Ultraviolet absorber UV-0) occupies the hydrophobic pocket of MD2 and blocks the dimerization of TLR4. 2,4′-Dihydroxybenzophenone inhibits the LPS induced mtROS production, and LPS induced inflammatory response by downregulating pro-inflammatory mediators and decreasing the expression of MyD88, p-IRAK4, and NF-κB. 2,4′-Dihydroxybenzophenone is also a UV absorber .
Cat. No.: HY-173008
YTHDF2-IN-1 (Compound CK-75) is a selective YTHDF2 inhibitor (Kd = 26.2 μM). YTHDF2-IN-1 binds to a small hydrophobic pocket on the YTH domain of YTHDF2, disrupting the interaction between YTHDF2 and m 6A-modified RNA. YTHDF2-IN-1 induces cell cycle arrest and Apoptosis. YTHDF2-IN-1 is applicable to research on chronic myeloid leukemia, colon cancer and choriocarcinoma .
Cat. No.: HY-D1190
CAS No.: 198696-03-6
Cat. No.: HY-N15451
CAS No.: 112515-42-1
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PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
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EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .
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LT175, a dual PPARα/γ ligand, is an orally active partial agonist against PPARγ(hPPARα:EC50=0.22 μm; mPPARα:EC50=0.26 μm; hPPARγ:EC50=0.48 μm). LT175 interacts with PPARγ and affects the recruitment of the coregulators cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1). LT175 interacts with PPARγ in a hydrophobic region called “diphenyl pocket”. LT175 has potent insulin-sensitizing effects and reduced adipogenic properties .
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-146814
CAS No.: 2687245-05-0
EBOV/MARV-IN-3 (compound 32) is a potent EBOV and MARV inhibitor with IC50 values of 0.5, 1.2 µM, respectively. EBOV/MARV-IN-3 binds to the hydrophobic pocket close to EBOV Y517. EBOV/MARV-IN-3 shows antiviral activity .
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BVDV-IN-1 is a non-nucleoside inhibitor (NNI) of bovine viral diarrhea virus (BVDV), with an EC50 of 1.8 μM. BVDV-IN-1 directly binds to a hydrophobic pocket of the BVDV RdRp. BVDV-IN-1 has antiviral activity against BVDV resistant to NNI thiosemicarbazone (TSC) .
Cat. No.: HY-162512
CAS No.: 81430-62-8
CB-0821 is a high affinity CCR5 inhibitor with a Ki of 0.04 nM. CB-0821 binds efficiently to the hydrophobic pocket of the CCR5 protein, to inhibit the interactions between viral protein and CCR5, thereby inhibiting viral entry. CB-0821 has the potential for anti-HIV research .
Cat. No.: HY-164523
CAS No.: 1093793-11-3
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PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .
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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
