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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>
R-R-3023 Antineoplaston A10 CAS No.91531-30-5 Antineoplaston A10/CAS No.91531-30-5, a naturally occurring substance in human body, is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. price>
R-C-1324 AZ7371 CAS:1494675-86-3 AZ 7371 is a non-covalent inhibitor of decaprenylphosphoryl-β-D-ribose 2-epimerase(DprE1;IC50=10nM),an enzyme involved in mycobacterial cell wall biogenesis.1 It inhibits wild-type M.smegmatis DprE1 and DprE1 harboring the drug-resistance mutation C394G(IC50=0.01 µM for both)but not the Y321H mutation (IC50=>10 µM). price>
R-R-3024 KRpep-2d CAS No.2098181-84-9 KRpep-2d/CAS No.2098181-84-9 is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research. price>
R-C-1325 AVN-944 (VX-944) CAS:297730-17-7 AVN-944(VX-944)is an orally available,synthetic small molecule with potential antineoplastic activity.AVN944 inhibits inosine monosphosphate dehydrogenase (IMPDH),an enzyme involved in the de novo synthesis of guanosine triphosphate (GTP),a purine molecule required for DNA and RNA synthesis.Inhibition of IMPDH deprives cancer cells of GTP,resulting in disruption of DNA and RNA synthesis, inhibition of cell proliferation,and the induction of apoptosis.AVN944 appears to have a selective effect on cancer cells in that deprivation of GTP in normal cells results in a temporary slowing of cell growth only.IMPDH is overexpressed in some cancer cells,particularly in hematological malignancies. price>
R-R-3025 MLS000532223 CAS No.16616-39-0 MLS000532223/CAS No.16616-39-0 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases. price>
R-C-1326 EHop-016 CAS:1380432-32-5 EHop-016 is a potent and selective Rac GTPase Rac1 and Rac3 inhibitor.EHop-016 inhibits Rac1 activity with an IC50 of 1.1 μM in MDA-MB-435 cells. EHop-016 inhibits Vav2 interaction with Rac,Rac-activated PAK1,lamellipodia formation,and cell migration. price>
R-R-3026 RAS/RAS-RAF-IN-1 CAS No.2447039-81-6 RAS/RAS-RAF-IN-1/CAS No.2447039-81-6 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity. price>