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R-R-3013 ASP2453 CAS No.2241719-73-1 ASP2453/CAS No.2241719-73-1 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM. price>
R-C-1314 AMG337 CAS:1173699-31-4 AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor.AMG 337 inhibits MET kinase activity with an IC50 of<5nM in enzymatic assays. price>
R-R-3014 Y16 CAS No.429653-73-6 Y16/CAS No.429653-73-6 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM. Y16 is active in blocking the interaction of LARG and related G-protein-coupled Rho GEFs with RhoA. Y16 shows no detectable effect on other diffuse B-cell lymphoma (Dbl) family Rho GEFs, Rho effectors, or a RhoGAP. price>
R-C-1315 RG2833 (RGFP109) CAS:1215493-56-3 RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3,respectively.The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively. price>
R-R-3015 K-Ras(G12C) inhibitor 12 CAS No.1469337-95-8 K-Ras(G12C) inhibitor 12/CAS No.1469337-95-8 is a K-Ras(G12C) inhibitor, the half-maximum effective concentration (EC50) for K-Ras(G12C) inhibitor 12 in H1792 cells is 0. price>
R-C-1316 GSK0660 CAS:1014691-61-2 GSK0660 is a potent PPARβ/δ antagonist with a pIC50 of 6.8(binding assay IC50 =155 nM;antagonist assay IC50=300nM)and is nearly inactive on PPARα and PPARγ with IC50s above approximately 10 μM.GSK0660(100nM)reduces CPT1a(a PPARβ/δ target gene)expression below the basal vehicle-treated level by approximately 50%,but shows no effect on PDK4 expression,which is also a PPARβ/δ target gene in skeletal muscle cells.GSK0660(0.5μM)reduces the levels of AMPK and eNOS phosphorylation,and BMP-2,Runx-2 mRNA expression in MC3T3-E1 cells. price>
R-R-3016 KRas G12R inhibitor 1 KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research. price>
R-C-1317 APD597 (JNJ-38431055) CAS:897732-93-3 APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes,with EC50 of 46 nM for hGPR119.IC50 value: 46 nM(EC50)Target:hGPR119The design and synthesis of a second generation GPR119-agonist clinical candidate for the treatment of diabetes is described.APD597 was selected for preclinical development based on a good balance between agonist potency,intrinsic activity and in particular on its good solubility and reduced drug-drug interaction potential. price>
R-R-3017 ZT-12-037-01 CAS No.2328073-61-4 ZT-12-037-01/CAS No.2328073-61-4 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM. price>
R-C-1318 CH-223191 CAS:301326-22-7 CH223191 is a potent and specific aryl hydrocarbon receptor(AhR)antagonist. CH223191 can prevent 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor.2,3,7,8-Tetrachlorodibenzo-p-dioxin(TCDD)is a widespread environmental pollutant with many toxic effects,including endocrine disruption,reproductive dysfunction,immunotoxicity,liver damage,and cancer. CH223191 potently inhibits TCDD-induced AhR-dependent transcription.In addition,CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR.These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes,target genes of the AhR.CH-223191,may be a useful agent for the study of AhR-mediated signal transduction and the prevention of TCDD-associated pathology. price>
R-R-3018 KRAS G12D inhibitor 14 CAS No.2765254-39-3 KRAS G12D inhibitor 14/CAS No.2765254-39-3 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D. price>
R-C-1319 Helioxanthin 8-1 CAS: 840529-13-7 Helioxanthin 8-1 is an analogue of helioxanthin,exhibites significant in vitro anti-HBV/HCV/HSV-1/HIV activity with EC50 of >5/10/1.4/15 uM. price>
R-R-3019 XRP44X CAS No.729605-21-4 XRP44X/CAS No.729605-21-4 inhibits Ras-induced transcription activation with the IC50 of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules. price>
R-C-1320 CB5083 CAS:1542705-92-9 CB-5083 is a novel first in class,potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models. price>
R-R-3020 SAH-SOS1A TFA CAS No.2896737-31-6 SAH-SOS1A TFA/CAS No.2896737-31-6 is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS. price>
R-C-1321 SYM2206 CAS:173952-44-8 SYM2206 is a potent and non-competitive AMPA receptor antagonist,with an IC50 of 1.6 μM.SYM2206 blocks Nav1.6-mediated persistent currents. price>
R-R-3021 AZD4625 AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRASG12C. AZD4625 has high oral bioavailability. price>
R-C-1322 Brigatinib (AP26113) CAS:1197953-54-0 Brigatinib,also known as AP-26113,is an orally active,potent and selective Dual ALK/EGFR inhibitor.AP26113 binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms.This leads to the inhibition of ALK kinase and EGFR kinase,disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells.In addition,AP26113 appears to overcome mutation-based resistance.ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development;ALK dysregulation and gene rearrangements are associated with a series of tumors. EGFR is overexpressed in a variety of cancer cell types. price>
R-R-3022 Z62954982 CAS No.1090893-12-1 Z62954982 (ZINC08010136)/CAS No.1090893-12-1 is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA). price>
R-C-1323 NSC59984 CAS:803647-40-7 NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway.The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells,with EC50 of 8.38 uM for p53-null HCT116 cells. price>