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INCB018424 (Ruxolitinib)

Catalog No. A11041
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JAK1/2 抑制剂

INCB018424 (Ruxolitinib)是有效和选择性的Janus相关激酶JAK1/2抑制剂，对JAK1，JAK2和JAK3的IC50分别为2.7、4.5和332 nM。了解更多

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. Combined inhibition of JAK2-STAT3 and SMO-GLI1/tGLI1 pathways suppresses breast cancer stem cells, tumor growth, and metastasis, Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. IL6/STAT3 Signaling Hijacks Estrogen Receptor α Enhancers to Drive Breast Cancer Metastasis, Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. JAK2V617F+ myeloproliferative neoplasm clones evoke paracrine DNA damage to adjacent normal cells through secretion of lipocalin-2., Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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TAK-875 (Fasiglifam)

Catalog No. A11018
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GPR 激动剂

TAK-875 (Fasiglifam)是一种有效的，选择性的GPR40激动剂。了解更多

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- Ying Liu, .et al. A synthetic free fatty acid-regulated transgene switch in mammalian cells and mice, Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. Mechanistic insights into the detection of free fatty and bile acids by ileal glucagon-like peptide-1 secreting cells, Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. Potentiation of Glucose-stimulated Insulin Secretion by the GPR40-PLC-TRPC Pathway in Pancreatic β-Cells, Sci Rep, 2016, 6: 25912 PMID: 27180622
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Cediranib (AZD2171)

Catalog No. A10185
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VEGFR 抑制剂

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂，此外对c-Kit和PDGFRβ也具有相似的抑制活性，对VEGFR的选择性比PDGFR-α，CSF-1R和Flt3分别高36倍，110倍和1000倍以上。了解更多

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- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
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SB 431542

Catalog No. A10826
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TGF-beta/Smad 抑制剂

SB 431542是转化生长因子-β超家族I型激活素受体样激酶（ALK）受体ALK4，ALK5和ALK7的有效抑制剂。了解更多

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- Huong Pham, .et al. BMP11 Negatively Regulates Lipid Metabolism in C2C12 Muscle Cells, Biotechnol Bioprocess Eng, 2020, ID: 222137835
- Tamara Chamberlin, .et al. Obesity Reduces Mammary Epithelial Cell TGFβ1 Activity Through Macrophage-Mediated Extracellular Matrix Remodeling, FASEB J, 2020, Jun;34(6):8611-8624 PMID: 32359100
- Satoshi Endo, .et al. Flavonol glycosides of Rosa multiflora regulates intestinal barrier function through inhibiting claudin expression in differentiated Caco-2 cells, Nutr Res, 2019, 4 November
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Vinflunine Tartrate

Catalog No. A10975
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Microtubule Associated 抑制剂

Vinflunine Tartrate是长春氟宁的酒石酸盐，它使微管不稳定，IC50为18.8 nM，并在细胞分裂过程中干扰微管的动力学。了解更多

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PIK-293

Catalog No. A10727
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PI3K 抑制剂

PIK-293是PI3-K抑制剂。PIK-293抑制p110α，p110β，p110δ。PIK-293是PIK-294的母体化合物。了解更多

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PIK-294

Catalog No. A10728
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PI3K 抑制剂

PIK-294是PI3激酶抑制剂，其效力比母体化合物PIK-293高20至60倍。它是已报道的最有效的p110δ选择性抑制剂之一。了解更多

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Cefditoren pivoxil

Catalog No. A10188
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Cefditoren pivoxil是口服的第三代头孢菌素抗生素。了解更多

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Bethanechol chloride

Catalog No. A10180
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Muscarinic receptor 激动剂

Bethanechol chloride是拟副交感神经的胆碱氨基甲酸酯，可选择性刺激毒蕈碱受体，而不会对烟碱样受体产生任何影响。了解更多

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Carmofur

Catalog No. A10183
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Carmofur是用作抗肿瘤药的嘧啶类似物。它是氟尿嘧啶的衍生物。了解更多

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Cefdinir

Catalog No. A10187
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Antibacterial

Cefdinir是第三代口服头孢菌素抗生素。了解更多

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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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Butenafine HCl

Catalog No. A11829
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Butenafine Hydrochloride是一种抗真菌药，可用于控制皮肤真菌感染，例如运动员的足癣和癣菌。了解更多

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JZL184

Catalog No. A12747
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MAGL 抑制剂

JZL184是一种有效的选择性单酰基甘油脂肪酶（MAGL）抑制剂。体内阻断内源性大麻素2-花生四烯酸甘油酯（2-AG）的水解（IC50 = 8 nM）。了解更多

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- Lakhan S Khara, .et al. Inhibiting the endocannabinoid degrading enzymes FAAH and MAGL during zebrafish embryogenesis alters sensorimotor function, J Exp Biol, 2022, May 1;225(9):jeb244146 PMID: 35438163
- Md Shah Sufian, .et al. Early suppression of the endocannabinoid degrading enzymes FAAH and MAGL alters locomotor development in zebrafish, J Exp Biol, 2021, 21 JUNE
- Toshihiko Tsutsumi, .et al. Identification of human glycerophosphodiesterase 3 as an ecto phospholipase C that converts the G protein-coupled receptor 55 agonist lysophosphatidylinositol to bioactive monoacylglycerols in cultured mammalian cells, Biochim Biophys Acta Mol Cell Biol Lipids, 2020, Sep;1865(9):158761 PMID: 32629025
- Rea Pihlaja, .et al. The Anti-Inflammatory Effects of Lipoxygenase and Cyclo-Oxygenase Inhibitors in Inflammation-Induced Human Fetal Glia Cells and the Aβ Degradation Capacity of Human Fetal Astrocytes in an Ex vivo Assay, Front Neurosci, 2017, 11: 299 PMID: 28611577