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R-C-1352 THZ1 CAS:1604810-83-4 THZ1 is a selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM.THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression. price>
R-R-3052 KRAS G12C inhibitor 28 CAS No.2649004-88-4 KRAS G12C inhibitor 28/CAS No.2649004-88-4 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1). price>
R-C-1353 Ezatiostat CAS:168682-53-9 Ezatiosta(TER199,TLK199,Telintra),a tripeptide analog of glutathione,is a peptidomimetic inhibitor of Glutathione S-transferase P1-1(GSTP1-1).Ezatiostat activates c-Jun NH2 terminal kinase(JNK1)and ERK1/ERK2 and induces apoptosis. price>
R-R-3053 (R)-CE3F4 CAS No.1593478-56-8 (R)-CE3F4/CAS No.1593478-56-8 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM). (R)-CE3F4 is more potent than racemic CE3F4 and (S)-CE3F4. price>
R-C-1354 Losartan Carboxylic Acid (EXP-3174) CAS:124750-92-1 Losartan Carboxylic Acid(E-3174),an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1(AT1)antagonist.The Ki values are 0.97,0.57,0.67 nM for rat AT1B/AT1A and human AT1,respectively.Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells(VSMC).Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure. price>
R-R-3054 KRAS G12D inhibitor 1 CAS No.2621928-43-4 KRAS G12D inhibitor 1 (example 243)/CAS No.2621928-43-4 is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation. KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. price>
R-C-1355 MK7622 CAS:1227923-29-6 MK-7622 is a muscarinic M1 receptor positive allosteric modulator.Target:M1 receptorMK-7622 is useful in the treatment of diseases in which the M1 receptor is involved,such as Alzheimer is disease,schizophreniapain or sleep disorders. price>
R-R-3055 PHT-7.3 CAS No.1614225-93-2 PHT-7.3/CAS No.1614225-93-2 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity. price>
R-C-1356 Ro 61-8048 CAS No. 199666-03-0 Ro61-8048 is a potent Kynurenine hydroxylase inhibitor(Ki=4.8 nM,IC50=37nM).Ro 61-8048 improves dystonia in a genetic model of paroxysmal dyskinesia.Ro 61-8048 may be potentially useful for the treatment of dyskinesias.Ro 61-8048 could be a new avenue to reduce neuronal loss in brain ischemia. price>
R-R-3056 SOS1-IN-11 CAS No.2654741-64-5 SOS1-IN-11/CAS No.2654741-64-5 is a potent SOS1 inhibitor with an IC50 value of 30 nM. price>
R-C-1357 AZD3965 CAS No. 1448671-31-5 AZD3965 is a selective inhibitor of monocarboxylate transporter 1(MCT1)with a binding affinity of 1.6 nM,is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.In vivo,AZD3965 is well tolerated and induces a dose and time dependent accumulation of lactate in the tumours,suppresses tumour growth and in the Raji model potentiates the effects of Rituxan,doxorubicin and bendamustine. The selective inhibition of lactate transport by the MCT1 inhibitor AZD3965 offers an novel mechanism for targeting the metabolic phenotype in tumours that preferentially express MCT1. price>
R-R-3057 CMC2.24 CAS No.1255639-43-0 CMC2.24 (TRB-N0224)/CAS No.1255639-43-0, an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis. price>
R-C-1358 KS176 CAS No. 1253452-78-6 KS176 is a potent and selective inhibitor of the breast cancer resistance protein(BCRP)multidrug transporter(IC50 values are 0.59 and 1.39 μM in Pheo A and Hoechst 33342 assays respectively).Displays no inhibitory activity against P-gp or MRP1. price>
R-R-3058 Kras4B G12D-IN-1 CAS No.2042365-85-3 Kras4B G12D-IN-1/CAS No.2042365-85-3 is a Kras4B G12D inhibitor with anticancer effects. Kras4B G12D-IN-1 decreases Kras protein expression in mouse embryonic fibroblasts (MEF) expressing Kras4B G12D (WO2016179558A1, Comp 994566). price>
R-C-1359 PD168393 CAS No. 194423-15-9 PD168393 is a potent,selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2.PD168393 irreversiblely inactivates EGF receptor(IC50=0.7 nM)and is inactive against insulin receptor,PDGFR,FGFR and PKC. price>
R-R-3059 Ketoconazole-d4 CAS No.1398065-75-2 Ketoconazole-d4/CAS No.1398065-75-2 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor. price>
R-C-1360 GSKJ4HCL CAS No. 1797983-09-5 GSK-J4 is a cell permeable,potent and selective histone demethylase.GSK-J4 is a prodrug of GSK J1,which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.GSK-J4 is used to probe the consequences of demethylation of H3K27me3.GSK-J4 inhibits the lipopolysaccharide-induced production of cytokines,including pro-inflammatory tumour necrosis facto(TNF). price>
R-R-3060 Atrovastatin-PEG3-FITC CAS No.1440755-31-6 Atrovastatin-PEG3-FITC (compound S31)/CAS No.1440755-31-6 is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay. price>
R-C-1361 SC66 CAS:871361-88-5 SC66 is a novel and potent AKT inhibitor,which reduced cell viability in a dose- and time-dependent manner,inhibited colony formation and induced apoptosis in HCC cells.SC66 treatment led to a reduction in total and phospho-AKT levels. SC66 significantly potentiated the effects of both conventional chemotherapeutic and targeted agents,doxorubicin and everolimus,respectively.In vivo,SC66 inhibited tumor growth of Hep3B cells in xenograft models,with a similar mechanism observed in the in vitro model.SC66 had antitumor effects on HCC cells. price>
R-R-3061 Ketoconazole-d8 CAS No.1217706-96-1 Ketoconazole-d8/CAS No.1217706-96-1 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor. price>