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R-R-2135 ZX-29 CAS No.2254805-62-2 ZX-29/CAS No.2254805-62-2 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect. price>
R-C-436 Dapagliflozin(BMS5121458) Dapagliflozin(BMS512148)is a selective,orally active inhibitor of the renal sodium-glucose co-transporter type 2(SGLT2)is in development for the treatment of type 2 diabetes mellitus.Dapagliflozin inhibits subtype 2 of SGLT2 which are responsible for at least 90% of the glucose reabsorption in the kidney.Blocking this transporter mechanism causes blood glucose to be eliminated through the urine.In clinical trials,dapagliflozin lowered HbA1c by 0.90 percentage points when added to metformin. price>
R-R-2136 BOLD-100 free base CAS No.783324-98-1 BOLD-100 (NKP-1339; IT-139) free base/CAS No.783324-98-1 is a ruthenium-based anticancer agent. BOLD-100 free base also is an inhibitor of stress-induced GRP78 upregulation, disrupting endoplasmic reticulum (ER) homeostasis and inducing ER stress and unfolded protein response (UPR). BOLD-100 free base interferes with the complex interplay between ER-stress response, lysosome dynamics, and autophagy execution.The free form of the compound is prone to instability, it is advisable to consider the stable salt form (BOLD-100) that retains the same biological activity. price>
R-C-437 Telaprevir (VX-950) Trapivir is an effective and selective reversible HCV NS3-4A protein inhibitor, which acts on NS3 protease domain and NS4A cofactor peptide of genotype 1(strain h).Vx-950 is an effective and selective peptide like inhibitor of hepatitis C virus NS3-4A serine protease.It shows excellent antiviral activity in both type 1b HCV replicon cells (50% inhibition concentration [IC50]=354nm) and human fetal liver cells(IC50=280nm) infected with sera from type 1A HCV positive patients. price>
R-R-2137 TSPO ligand-1 CAS No.4560-08-1 TSPO ligand-1/CAS No.4560-08-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration. price>
R-C-438 Telatinib (BAY 57-9352) Telatinib has low affinity for Raf kinase pathway,epidermal growth factor receptor family,fibroblast growth factor receptor(FGFR) family or Tie-2 receptor.Tiratinib is metabolized by a variety of cytochrome P450 (CYP) subtypes, including CYP3A4/3A5,cyp2c8, CYP2C9 and CYP2C19,as well as uridine diphosphate glucuronosyltransferase 1A4 (ugt1a4).The formation of N-glucuronide is the main biotransformation pathway of tiratinib. price>
R-R-2138 Trimetazidine-d8 dihydrochloride CAS No.1219795-37-5 Trimetazidine-d8 (dihydrochloride)/CAS No.1219795-37-5 is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor. price>
R-C-439 gsk1904529A Gsk-1904529a is an IGF-1R inhibitor,which has broad application prospects in the treatment of igf-ir-dependent tumors.Gsk1904529a selectively inhibited IGF-IR and IR with IC50 of 27 and 25 nmol/L,respectively.Gsk1904529a blocks autophosphorylation and downstream signal transduction of receptor,leading to cell cycle arrest.It inhibits the proliferation of cell lines from solid and hematological malignancies.Multiple myeloma and Ewing sarcoma cell lines are the most sensitive. price>
R-R-2139 PI-1840 CAS No.1401223-22-0 PI-1840/CAS No.1401223-22-0 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α. price>
R-C-440 LY2157299 Galunisertib(LY2157299)is selective TGF-receptor kinase inhibitor.Galunisertib was found to inhibit the growth in an in vitro clonogenic assay in 6.3%(5/79)of the examined PDX. price>
R-R-2140 CUR5g CAS No.1370032-20-4 CUR5g/CAS No.1370032-20-4 is a potent autophagy inhibitor. CUR5g selectively inhibits autophagosome degradation in cancer cells by blocking autophagosome-lysosome fusion. CUR5g blocks the recruitment of STX17 to autophagosomes via a UVRAG-dependent mechanism, resulting in the inability of autophagosomes to fuse with lysosomes. CUR5g improves the anticancer effect of Cisplatin (HY-17394) against A549 cells both in vitro and in vivo. price>
R-C-441 DMXAA(AS1404,ASA404) DMXAA is an apoptosis inducer,and an anti-vascular.DMXAA is an inhibitor of NQO1, Flk-1 and Flt-1. price>
R-R-2141 GW406108X CAS No.1644443-92-4 GW406108X/CAS No.1644443-92-4 is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK. price>
R-C-442 Brivanib(bms-540215) Brivanib is an ATP-competitive inhibitor against human Flk-1(VEGFR-2)and mouse Flk-1 with IC50 of 25 nM and 89 nM,respectively.Brivanib also inhibits Flt-1 (VEGFR-1)and Flg (FGFR-1) with IC50 of 0.38 and 0.148 μM.Brivanib displays antitumor activities in H3396 xenograft.This compound completely inhibits the tumor growth,with TGI of 85% and 97%, respectively. price>
R-R-2142 Manzamine A hydrochloride CAS No.104264-80-4 Manzamine A hydrochloride/CAS No.104264-80-4, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A hydrochloride targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A hydrochloride has antimalarial and anticancer activities. Manzamine A hydrochloride also shows potent activity against HSV-1. price>
R-C-443 Brivanib alaninate(BMS-582664) Brivanib Alaninate is the alaninate salt of a vascular endothelial growth factor receptor 2(VEGFR2) inhibitor with potential antineoplastic activity.Brivanib strongly binds to and inhibits VEGFR2,a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells;inhibition of VEGFR2 may result in inhibition of tumor angiogenesis,inhibition of tumor cell growth,and tumor regression. price>
R-R-2143 Vacuolin-1 CAS No.351986-85-1 Vacuolin-1/CAS No.351986-85-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells. price>
R-C-444 vx-702 VX-702 inhibits p38 MAPK, preventing p38 MAPK-dependent inflammatory cytokine release.VX-702 is in development to treat inflammation and cardiovascular diseases and currentlyshows mixed results in clinical trials as a potential treatment for rheumatoid arthritis.In vitro,Vx-702 decreases platelet lesioning in storage without affecting platelet function. price>
R-R-2144 Gefitinib-d3 CAS No.1173976-40-3 Gefitinib-d3 (ZD1839-d3)/CAS No.1173976-40-3 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity. price>
R-C-445 Linifanib (ABT-869) Linifanib(ABT-869) is a novel,potent ATP-competitive VEGFR/PDGFR inhibitor for KDR(IC50:4 nM),CSF-1R (IC50:3 nM),Flt-1/3(IC50:3/4 nM)and PDGFRβ(IC50:66 nM).Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases,such as FMS-related tyrosine kinase receptor-3 (FLT3). price>