Search results for: 'alz 801'
Catalog No.
Product Name
Application
Product Information
Product Citation
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NMDA receptor antagonist
(+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM. -
NMDA receptor antagonist.
(-)-MK 801 maleate acts as a potent, selective, and non-competitive NMDA receptor antagonist. It acts by binding to a site located within the NMDA associated ion channel. -
GSK-3β inhibitor
Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM). -
anti-inflammatory (NSAID) agent
Ibuprofen piconol is a non-steroidal, anti-inflammatory (NSAID) agent for the topical relief of primary thermal burns and sunburns. - DL-threo-2-methylisocitrate is a substrate of isocitrate lyase 1(ICL1).
- N4-Acetylcytidine triphosphate is efficiently used as a substrate in T7 Polymerase-catalyzed in vitro transcription and can be incorporated into multiple templates.
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BCR-ABL inhibitor
AP24534 (Ponatinib) is a potent multi-kinase and pan-BCR-ABL inhibitor.- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. , Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. , Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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Muscarinic receptor agonist
Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors. -
Antiviral agent
Famciclovir(BRL 42810) is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections. - Rsogladine is an anti-gastric ulcer agent that facilitates gap-junctional intercellular communication through M1 muscarininc acetylcholine receptor binding.
- Ranolazine is a partial fatty acid oxidation inhibitor, shifts ATP production from fatty acid to more oxygen-efficient carbohydrate oxidation.
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RTK inhibitor
Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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HCV Protease inhibitor
VX-222 is a small molecule non-nucleoside inhibitor of HCV NS5B polymerase that is being investigated for the treatment of hepatitis C virus infection.- Wataru Ito, .et al. , Antivir Chem Chemother, 2015, Dec; 24(5-6): 148-154 PMID: 27503576
- Hui Shen, .et al. , PLoS One., 2013, 8(12): e82299 PMID: 24358168
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MDR1/P-gp Inhibitor
PSC-833 is a kind of P-glycoprotein (P-gp) modulator that inhibits P-gp-mediated multidrug-resistance (MDR).- Somin Lee, .et al. , Methods Mol Biol, 2022, 2492:251-263 PMID: 35733049
- Somin Lee, .et al. , Biotechnol Bioeng, 2019, 10 November
- Somin Lee, .et al. , bioRxiv, 2018, Nov. 18
- Watanabe N, .et al. , Biopharm Drug Dispos, 2018, Jan;39(1):30-37 PMID: 29055041
- Higashi H, .et al. , Biol Pharm Bull, 2017, 40(8):1314-1319 PMID: 28769012
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Hedgehog signaling activator
Purmorphamine is a 2,6,9-trisubstituted purine that promotes the differentiation of both human and mouse mesenchymal progenitor cells into osteoblasts.- Mark van den Hurk, .et al. , NPJ Parkinsons Dis, 2022, Oct 18;8(1):134 PMID: 36258029
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HCV NS3/4A protease inhibitor
Simeprevir is a potent inhibitor of HCV NS3/4A protease (Ki = 0.36 nM) and viral replication (replicon EC50 = 7.8 nM). -
PPARγ agonist
Pioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α. -
5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
- TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
- Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.
- Fmoc-Val-Cit-PAB-PNP is a cleavable peptide linker, is a linker for antibody-drug-conjugation (ADC).
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rRNA biogenesis inhibitor
Quarfloxin (CX-3543) is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.- Janne J. M. van Schie, .et al. , Nat Commun, 2020, 11: 4287 PMID: 32855419
- Yue Sheng, .et al. , Blood, 2020, Aug 21 PMID: 32822452
- Hald øH, .et al. , Oncogene, 2018, Dec 12 PMID: 30542116
- Louise E. Kerry, .et al. , PLoS Negl Trop Dis, 2017, Mar; 11(3): e0005432 PMID: 28263991
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FAK inhibitor
PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.- Dai Sonoda, .et al. , Oncol Rep, 2022, Jan;47(1):19 PMID: 34796907
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Neutrophil elastase inhibitor
Freselestat is a potent neutrophil elastase inhibitor. Freselestat reduces inflammatory mediators during simulated extracorporeal circulation. ONO-6818 significantly reduced interleukin 8 and C5b-9 production. ONO-6818 did not modulate changes of CD11b and L-selectin during recirculation. - Sapacitabine is an orally bioavailable pyrimidine analogue prodrug with potential antineoplastic activity.
- Sally L George, .et al. , EBioMedicine, 2020, Aug 23;59:102971 PMID: 32846370
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Adrenergic Receptor agonist
Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels. -
HSV inhibitor
ASP2151, is a herpes virus helicase-primase inhibitor. ASP2151 had significantly better anti-HSV activity against herpes simplex keratitis than valacyclovir and acyclovir after systemic or topical use. -
CCR 2 antagonist
Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively. -
Bcl-2 Inhibitor
Bcl-2 Inhibitor contains a mixture of two tautomers. A potent, cell-permeable, Bcl-2 inhibitor competes with Bak BH3 peptide for binding to Bcl-2 and Bcl-XL in vitro (IC50 =10 uM and 7 uM, respectively).- Toshiyuki Sumi, .et al. , Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
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NK1 receptor antagonist
Rolapitant, also known as SCH-619734, is a selective, bioavailable, CNS penetrant neurokinin NK1 receptor antagonist that shows behavioral effects in animals models of emesis.- Bubak AN, .et al. , J Infect Dis, 2018, Sep 8;218(8):1324-1335 PMID: 29788447
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DNA topoisomerase II inhibitor
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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beta-lactamase inhibitor
Durlobactam, also known as ETX2514, is a beta-lactamase inhibitor drug candidate. -
prostacyclin receptor agonist
NS-304 is a selective prostacyclin IP1 receptor agonist (Ki values are 260 and 2100 nM and for human and rat IP receptors, and >10 μM for EP1-4, DP, FP, and TP receptors). -
DPP-4 inhibitor
Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. -
LPA1 Receptor antagonist
AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively -
BMI-1 inhibitor
PTC-209 HBr is the hydrobromide salt of PTC-209. PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
- 5,15-Diacetyl-3-benzoyllathyrol, extracted from Euphorbiaceae Euphorbia lathyris dry mature seeds.
- Isomangiferin is found in fruits. Isomangiferin is a constituent of Mangifera indica (mango).
