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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
40 Results for "
Small molecule antagonist
" in MedChemExpress (MCE) Product Catalog:
Products (40)
40 Results for "Small molecule antagonist" in MCE Product Catalog:
2
2 Cited Publications
Synonyms: BMS-986177; JNJ-70033093
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Milvexian is an orally bioavailable, small-molecule, reversible, direct antagonists of factor Xia, with the Ki of 0.11, 0.38, 0.64, 490, 350 nM for human, rabbit, dog, rat, mouse, respectively. Milvexian shows anti-thrombosis activity in vitro and in vivo, and can be used for thrombus study .
2
2 Cited Publications
Cat. No.: HY-19767
CAS No.: 1629249-33-7
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GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer .
2
2 Cited Publications
Cat. No.: HY-19767A
CAS No.: 1629249-40-6
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GSK 3008348 hydrochloride is a small molecule antagonist of integrin αvβ6 with IC50 values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer .
2
2 Cited Publications
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TLR7/8/9-IN-1 is a potent and orally bioavailable small molecule antagonist (IC50 = 43 nM) of Toll-like receptors 7/8/9 (TLR7/8/9).
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TRP Channel Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Keap1-Nrf2 Amyloid-β Fungal Apoptosis
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
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1
1 Cited Publications
Cat. No.: HY-159989
CAS No.: 3118919-69-7
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UNC10142 (Compound 44) is a first-in-class small molecule antagonist of CHD1 that binds with an IC50 value of 1.7 μM. UNC10142 leads to a dose-dependent reduction in viability in PTEN-deficient prostate cancer cells .
1
1 Cited Publications
Cat. No.: HY-172458
CAS No.: 473687-20-6
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Z-3578 is an orally active small-molecule antagonist of MrgX2 with potent antipseudoallergic activity, exhibiting a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppresses the release of β-hexosaminidase, significantly reduces the release of histamine and TNF-α, and decreases intracellular calcium flux. In a mouse pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation, and reduces serum histamine levels. Z-3578 can be used for the study of pseudoallergic reactions .
Cat. No.: HY-30004
CAS No.: 22059-21-8
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AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2 .
Cat. No.: HY-15001G
CAS No.: 1227633-49-9
Synonyms: SR1 (GMP)
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SYD5115 is an orally available TSH-R antagonist .
Cat. No.: HY-111308
CAS No.: 847554-50-1
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RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve agent addiction including selectively decrease self-administration .
Cat. No.: HY-18668
CAS No.: 593274-97-6
Integrin antagonist 27 (Compound 27) is a small molecule integrin αvβ3 antagonist with an affinity of 18 nM. Integrin antagonist 27 can be combined with Paclitaxel (HY-B0015) to selectively target αvβ3-positive metastatic cancer cells. Integrin antagonist 27 is used as an anticancer agent .
Cat. No.: HY-16994
CAS No.: 1801873-49-3
OICR-0547 is a negative control, closely related derivative of OICR-9429 (HY-16993). OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction. OICR-0547 is an inactive control compound that no longer binds to WDR5 .
Cat. No.: HY-125475
CAS No.: 927881-99-0
Synonyms: GMI-1070
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Rivipansel is a small-molecule glycomimetic pan-selectin antagonist with inhibitory activity against E-selectin and P-selectin. Rivipansel binds tightly to the lectin domain of E-selectin, and selectively blocks the recognition of CD62L by E-selectin without affecting the binding of PSGL-1 to E-selectin. Rivipansel functionally inhibits the adhesion of hematopoietic cells to endothelial cells, and is applicable to research related to sickle cell disease .
Cat. No.: HY-30004R
CAS No.: 22059-21-8
Cat. No.: HY-124072
CAS No.: 1186371-31-2
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HL001 is an orally active small molecule inhibitor of Cyclophilin A (CypA) and a receptor antagonist of Lysophosphatidic acid 1 (LPA1). HL001 induces cell cycle arrest and apoptosis of tumor cells by p53. HL001 stabilizes p53 by down-regulating G3BP1, inducing reactive oxygen species and DNA damage. HL001 disrupts the interaction between MDM2 and p53-72R in a CypA dependent manner. HL001 has antitumor activity. HL001 can also be used to study pulmonary fibrosis .
Cat. No.: HY-100224G
CAS No.: 304909-07-7
Cat. No.: HY-125836
CAS No.: 2206788-99-8
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CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
CCR4 antagonist 2 (Compound 31) exhibits IC50 values of Ca 2+flux and (chemotaxis) CTX are 40 nM and 70 nM, respectively .
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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
