308 Results for "

drug selectivity

" in MedChemExpress (MCE) Product Catalog:
Products (308)

308 Results for "drug selectivity" in MCE Product Catalog:

138
138 Publications Verification
Cat. No.: HY-15244
CAS No.: 1217486-61-7
Purity:  99.88%
Synonyms: BYL-719
Alpelisib (BYL-719) is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome .
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138
138 Publications Verification
Cat. No.: HY-15244A
CAS No.: 1584128-91-5
Synonyms: BYL-719 hydrochloride
Alpelisib (BYL-719) hydrochloride is an orally active PI3Kα-selective inhibitor that blocks the conversion of PIP2 to PIP3, thereby inhibiting pathways including PI3K/AKT/mTOR, MAPK/ERK, Notch and JAK-STAT. Alpelisib hydrochloride also induces apoptosis, G0/G1 phase arrest and senescence; it significantly inhibits the proliferation, self-renewal, stemness and epithelial-mesenchymal transition (EMT) of tumor cells, reduces cancer stem cell populations and decreases the expression of stem cell markers. Alpelisib hydrochloride not only enhances the sensitivity to Eribulin (HY-13442) and exerts a synergistic effect with Paclitaxel (HY-B0015), but may also induce drug resistance by upregulating the SGK3/GSK3β/β-catenin signaling pathway. Alpelisib hydrochloride can be applied to research related to breast cancer, gastric cancer and lipomas associated with PTEN hamartoma tumor syndrome .
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70
70 Cited Publications
Cat. No.: HY-14398
CAS No.: 169590-42-5
Purity:  99.89%
Synonyms: SC 58635
Celecoxib,a selective and BBB-permeable non-steroidal anti-inflammatory drug (NSAID), is a selective COX-2 inhibitor with an IC50 of 40 nM.
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26
26 Cited Publications
Cat. No.: HY-10127
CAS No.: 722543-31-9
Purity:  99.62%
Synonyms: AZD1152
Target:  

Aurora Kinase Apoptosis

Research Areas:  

Cancer

Barasertib (AZD1152), a pro-drug of Barasertib-hQPA, is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib (AZD1152) induces growth arrest and apoptosis in cancer cells .
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25
25 Cited Publications
Cat. No.: HY-15417
CAS No.: 110448-33-4
Purity:  99.60%
ML-7 hydrochloride is a selective and highly specific myosin light chain kinase (MLCK) inhibitor that acts as a trabecular meshwork (TM) relaxant. ML-7 hydrochloride enhances Quinocetone (HY-123581)-induced phosphorylation of ERK, p38 MAPK and JNK, attenuates Akt activation, and promotes apoptosis of hepatocellular carcinoma cells. ML-7 hydrochloride reduces Th2 cytokine secretion by inhibiting MLCK, while alleviating smooth muscle hyperplasia and collagen deposition . As a non-antibiotic adjuvant, ML-7 hydrochloride restores the sensitivity of drug-resistant bacteria to Tigecycline (HY-B0117) . ML-7 hydrochloride can be used in research related to glaucoma, hepatocellular carcinoma, asthma, and Klebsiella pneumoniae infection .
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5
5 Cited Publications
Cat. No.: HY-132258A
CAS No.: 1453084-37-1
Purity:  99.71%
Synonyms: IMGN853 (solution)
Research Areas:  

Cancer

Mirvetuximab soravtansine (IMGN853) solution is an anti-folate receptor α (FRα) antibody drug-conjugate (ADC) consisting of the cytotoxic maytansinoid, DM4, covalently linked to the humanized monoclonal antibody M9346A, and the drug-linker conjugate for ADC is sulfo-SPDB-DM4 (HY-101141). Mirvetuximab soravtansine selectively binds to folate receptor 1 (FOLR1). Mirvetuximab soravtansine has an anti-proliferative effect via growth arrest and augmented DNA damage .
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5
5 Cited Publications
Cat. No.: HY-B1153
CAS No.: 3820-67-5
Synonyms: Glafenin
Glafenine (Glafenin) is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF) .
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5
5 Cited Publications
Cat. No.: HY-B1153A
CAS No.: 65513-72-6
Synonyms: Glafenin hydrochloride
Glafenine (Glafenin) hydrochloride is a non-selective, non-steroidal anti-inflammatory drug-based COX-1/COX-2 inhibitor. Glafenine hydrochloride exerts anti-inflammatory, anti-proliferative and anti-cell migration effects by inhibiting the arachidonic acid metabolic pathway and reducing prostaglandin synthesis. Glafenine hydrochloride can induce cell cycle arrest in vascular smooth muscle cells and endothelial cells and reduce the synthesis of the extracellular matrix protein Tenascin. Glafenine hydrochloride can be used in the research of inflammatory-related diseases, vascular restenosis and cystic fibrosis (CF) .
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4
4 Cited Publications
Cat. No.: HY-P1291
CAS No.: 201422-03-9
PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
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4
4 Cited Publications
Cat. No.: HY-P1291A
PKI 14-22 amide, myristoylated TFA is a selective, cAMP-dependent, competitive PKA inhibitor with Ki=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated TFA makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated TFA can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated TFA can prevent the development of analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated TFA can be used in research fields such as opioid tolerance mechanisms and antiviral drugs .
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4
4 Cited Publications
Cat. No.: HY-101126
CAS No.: 1361951-15-6
Purity:  99.96%
Synonyms: TP-3654
Research Areas:  

Cancer

Nuvisertib (TP-3654) is an orally active second-generation pan-PIM kinase inhibitor with Ki values of 5 nM, 239 nM, and 42 nM against PIM-1, PIM-2, and PIM-3, respectively. Nuvisertib inhibits JAK-independent inflammatory and survival signaling pathways, reduces the production of proinflammatory cytokines, restores apoptotic sensitivity, inhibits mTORC1, MYC, and TGF-β signaling pathways, and decreases the expression of fibrosis markers. Nuvisertib selectively impairs the transport function of ABCG2, resensitizes multidrug-resistant cancer cells to cytotoxic drugs, and overcomes JAK2 inhibitor resistance. Nuvisertib can be used in research related to myelofibrosis, renal cell carcinoma, multidrug-resistant cancer, advanced solid tumors, urothelial carcinoma, and prostate adenocarcinoma .
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4
4 Cited Publications
Cat. No.: HY-14674
CAS No.: 383432-38-0
Purity:  98.72%
Research Areas:  

Infection Cancer

CP-724714 is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection .
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2
2 Cited Publications
Cat. No.: HY-104086
CAS No.: 259886-50-5
Purity:  ≥98.0%
Synonyms: CB7; Carrier CB7
Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing.
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2
2 Cited Publications
Cat. No.: HY-B0494
CAS No.: 2438-72-4
Synonyms: Bufexamic acid
Target:  

HDAC Aminopeptidase

Research Areas:  

Inflammation/Immunology Cancer

Bufexamac is a selective Ⅱb HDAC (HDAC6, HDAC10) and LTA4H dual inhibitor, with Kds of 0.53 µM and 0.22 µM for HDAC6 and HDAC10. Bufexamac is a nonsteroida anti-inflammatory drug .
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2
2 Cited Publications
Cat. No.: HY-120824
CAS No.: 78967-07-4
Purity:  99.34%
Target:  

COX

Research Areas:  

Inflammation/Immunology

Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities .
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2
2 Cited Publications
Cat. No.: HY-106033
CAS No.: 204318-14-9
Purity:  98.15%
Synonyms: DOTATOC; SDZ-SMT 487; SMT 487
Research Areas:  

Cancer

Edotreotide is a ligand that selectively targets SSTR2 and can competitively bind to the receptor. Edotreotide mediates the targeted delivery, while modificated with radionuclides (such as 90Y, 177Lu, and 68Ga) to SSTR-positive tumors and induces tumor cell apoptosis by releasing β rays. Edotreotide has strong tumor targeting and precise killing activity. Edotreotide is used in the synthesis of radionuclide-drug conjugates (RDCs) and is widely used in the field of neuroendocrine tumors (such as metastatic carcinoids, lung and thymus NETs) .
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2
2 Cited Publications
Cat. No.: HY-W019823
CAS No.: 76204-02-9
4-MUNANA is a substrate of influenza virus neuraminidase (NA) with high selectivity and irreversible reaction. In the enzymatic reaction, 4-MUNANA is hydrolyzed by NA to generate fluorescent 4-methylumbelliferone (4-MU). By detecting the fluorescence intensity of 4-MU, quantitative analysis of NA activity can be achieved. 4-MUNANA can be used in influenza-related research, such as screening NA inhibitors, developing new anti-influenza drugs, and studying the infection mechanism of influenza viruses .
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2
2 Cited Publications
Cat. No.: HY-137433
CAS No.: 1835667-63-4
Purity:  99.86%
Synonyms: D-0316
Research Areas:  

Cancer

Befotertinib (D-0316) is an orally active EGFR inhibitor and ABCB1 inhibitor. Befotertinib selectively targets EGFR mutations including EGFR T790M, EGFR L858R and delE746-A750, forms covalent bonds with EGFR C797, inhibits oncogenic signaling pathways, and exerts antiproliferative effects. Befotertinib inhibits ABCB1-mediated drug efflux, activates the ATPase activity of ABCB1, acts as a chemosensitizer and apoptosis enhancer, and restores the sensitivity of multidrug-resistant cancer cells. Befotertinib can be used in research related to multidrug-resistant cancers and non-small cell lung cancer .
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1
1 Cited Publications
Cat. No.: HY-15349
CAS No.: 149488-17-5
Purity:  98.62%
Synonyms: LY300046
Research Areas:  

Infection

Trovirdine (LY300046) is a selective non-nucleoside HIV-1 reverse transcriptase inhibitor, with an IC50 value of 0.012 μM against the wild-type enzyme. Trovirdine inhibits the replication of both wild-type and mutant HIV-1, and exerts synergistic or additive effects when combined with some antiviral drugs. Trovirdine is applicable to research related to HIV-1 infection .
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1
1 Cited Publications
Cat. No.: HY-P10761
CAS No.: 2941391-49-5
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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