Search results for: 'ltx 401'
Catalog No.
Product Name
Application
Product Information
Product Citation
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DNA-PK inhibitor
Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM). - Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
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PTP1B Inhibitor
TCS 401 is a selective inhibitor of protein-tyrosine phosphatase 1B (PTP1B) (Ki values are 0.29, 59, 560, 1100, > 2000, > 2000 and > 2000 μM for PTP1B, CD45 D1D2, PTPβ, PTPε D1, SHP-1, PTPα D1 and LAR D1D2 respectively). -
GnRH antagonist
Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist. - MDRTB-IN-1 (5aα) is an antibiotic which is against Mycobacterium tuberculosis H37Rv with a MIC90 value of 10.5 μM.
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Caspase inhibitor
Z-VAD(OH)-FMK is an irreversible tripeptide inhibitor of all caspases. - Asparagine is one of the 20 most common natural amino acids on Earth.
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Telomerase Inhibitor
BIBR 1532 is a selective telomerase inhibitor (IC50 values are 93, > 100000 and > 100000 nM for human telomerase, human RNA polymerase I and human RNA polymerase II + III respectively).
- Hosoi T, .et al. , Neurosci Lett, 2016, Aug 26;629:241-244 PMID: 27443785
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Telomerase inhibitor
Costunolide is an Inhibitor of human telomerase activity (IC50 = 65 μM in MCF-7 breast cancer cells). It is described to act as an antioxidant, anti-mycobacterial, anti-inflammatory, and anti-viral, with cytotoxic activity. -
VEGFR Inhibitor
E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.- Mai Nakahara, .et al. , Biomed Rep, 2022, Aug 3;17(4):78 PMID: 36158319
- Paula Sagmeister, .et al. , J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Keisuke Enomoto, .et al. , Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Jindal A, .et al. , J Transl Sci, 2020, 7: 1-10
- Koide H, .et al. , Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. , Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
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nonsteroidal anti-inflammatory agent
Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. -
IGF-1R inhibitor
GSK1904529A selectively inhibits IGF-IR and IR with IC(50)s of 27 and 25 nmol/L, respectively. - Lubiprostone is a bicyclic fatty acid metabolite analog of Prostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, and increase gastrointestinal transit.
- Podophyllotoxin is a potent inhibitor of microtubule assembly that binds at the colchicine site of tubulin.
- Shikimic acid(Shikimate), more commonly known as its anionic form shikimate, is an important biochemical intermediate in plants and microorganisms.
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estrogen-receptor modulator
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 ?M and 2.6 ?M, respectively. -
MEK Inhibitor
TAK-733 is an orally bioavailable small-molecule inhibitor of MEK1 and MEK2 (MEK1/2) with potential antineoplastic activity.- Saeko Yoshioka, .et al. , Int J Tryptophan Res, 2022, Nov 30;15 PMID: 36467776
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CaSR antagonist
NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM. -
pan-Raf inhibitor
MLN 2480 is an oral, selective pan-Raf kinase inhibitor in chinical trials. -
Histamine Receptor antagonist
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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BET inhibitor
GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family - Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
- ENOblock (AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
- Rachel Polcyn, .et al. , Neurochem Int, 2020, Jul 7;104788 PMID: 32650031
- Yakarsonmez S, .et al. , Mol Divers, 2019, Nov 21 PMID: 31754915
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HDAC6 inhibitor
ACY-1215 selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. -
mGlu4 receptor modulator
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. - Butylphthalide is an antioxidant and one of the chemical constituents in celery oil, along with sedanolide, which is primarily responsible for the aroma and taste of celery.
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GPR4 antagonist
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. -
Topoisomerase I inhibitor
9-Aminocamptothecin is a topoisomerase I inhibitor with potent anticancer activity. -
MGAT3 inhibitor
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM. - Homogentisic acid is a specific metabolite in urine and serum, which is used for diagnosis of alkaptonuria.
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endothelin receptor modulator
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. - Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
- Muthulakshmi S, .et al. , J Appl Toxicol, 2018, Nov;38(11):1388-1397 PMID: 29923290
- Betonicine can be found in herbs and spices and pulses, which makes betonicine a potential biomarker for the consumption of these food products. Betonicine can be found primarily in urine. This compound belongs to the class of organic compounds known as l-alpha-amino acids.
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AMPA Receptor Blocker
IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors. -
NHE3 inhibitor
Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.- Kuniko Hunter, .et al. , Tissue Eng Part A, 2022, Nov 18 PMID: 36274231
- Xingjie Tan, .et al. , Authorea, 2022, May 25
- Kunyan Zhou, .et al. , Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. , Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. , Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. , Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. , Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. , Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. , Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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JAK3 inhibitor
Decernotinib is an oral, selective Janus kinase 3 (JAK3) inhibitor being developed by Vertex.
