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R-R-2956 Cysmethynil CAS No.851636-83-4 Cysmethynil/CAS No.851636-83-4 is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research. price>
R-C-1257 BIO CAS: 667463-62-9 BIO(GSK-3 Inhibitor IX,6-bromoindirubin-3-oxime,6-Bromoindirubin-3-oxime,MLS 2052)is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/βin a cell-free assay,shows>16-fold selectivity over CDK5,also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2.BIO induces apoptosis in human melanoma cells. price>
R-R-2957 N-Salicyloyltryptamine CAS No.31384-98-2 N-Salicyloyltryptamine/CAS No.31384-98-2 acts on voltage-dependent Na+, Ca2+, and K+ ion channels inhibitor. N-Salicyloyltryptamine inhibits K+ currents with an IC50 value of 34.6 μM (Ito). N-Salicyloyltryptamine also exhibits anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect-. price>
R-C-1258 ZLN005 CAS No. 49671-76-3 ZLN005 is a PGC-1α Transcriptional Regulator,which shoed some beneficialfEffects on diabetic db/db mice.ZLN005 increased fat oxidation and improved the glucose tolerance, pyruvate tolerance,and insulin sensitivity of diabetic db/db mice.Hyperglycemia and dyslipidemia also were ameliorated after treatment with ZLN005. price>
R-R-2958 Sotorasib CAS No.2296729-00-3 Sotorasib (AMG-510)/CAS No.2296729-00-3 is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors. price>
R-C-1259 MS436 CAS No. 1395084-25-9 MS436 is a BRD4 inhibitor.MS436,through a set of water-mediated interactions, exhibits low nanomolar affinity(estimated Ki of 30-50 nM).MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. price>
R-R-2959 MRTX1133 CAS No.2621928-55-8 MRTX1133/CAS No.2621928-55-8 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations. price>
R-C-1260 BRD4770 CAS:1374601-40-7 BRD4770 is a histone methyltransferase G9a inhibitor.BRD4770 reduces di- and trimethylation of lysine 9 on histone H3(H3K9)with an EC50 of 5 µM,and has less or little effect toward H3K27me3,H3K36me3,H3K4me3,and H3K79me3.BRD4770 can activate the ataxia telangiectasia mutated(ATM)pathway and induce cell senescence. price>
R-R-2960 BI-2865 CAS No.2937327-93-8 BI-2865/CAS No.2937327-93-8 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM). price>
R-C-1261 YL-109 CAS : 36341-25-0 YL-109 has ability to inhibit breast cancer cell growth and invasiveness in vitro and in vivo.YL-109 repressed the sphere-forming ability and the expression of stem cell markers in MDA-MB-231 mammosphere cultures.YL-109 increased the expression of carboxyl terminus of Hsp70-interacting protein(CHIP),which suppresses tumorigenic and metastatic potential of breast cancer cells by inhibiting the oncogenic pathway.YL-109 induced CHIP transcription because of the recruitment of the aryl hydrocarbon receptor(AhR)to upstream of CHIP gene in MDA-MB-231 cells.Consistently,the antitumor effects of YL-109 were depressed by CHIP or AhR knockdown in MDA-MB-231 cells.YL-109 inhibits cell growth and metastatic potential by inducing CHIP expression through AhR signaling and reduces cancer stem cell properties in MDA-MB-231 cells. price>
R-R-2961 BI-2852 CAS No.2375482-51-0 BI-2852/CAS No.2375482-51-0 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. price>
R-C-1262 GSK 525762A (I-BET-762) CAS:1260907-17-2 GSK-525762A is a small molecule inhibitor of the BET(Bromodomain and Extra-Terminal)family. price>
R-R-2962 BI-2493 CAS No.2937344-16-4 BI-2493/CAS No.2937344-16-4 is a structural analogue of BI-2865 and a highly selective pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research. price>
R-C-1263 AM251 CAS:183232-66-8 AM251 is a potent CB1 receptor antagonist(IC50=8 nM,Ki=7.49 nM)that displays 306-fold selectivity over CB2 receptors. price>
R-R-2963 LUNA18 CAS No.2676177-63-0 LUNA18/CAS No.2676177-63-0 is an orally active KRAS inhibitor with an IC50 of <2 nM against KRASG12D-SOS. LUNA18 can be used for the research of cancer. price>
R-C-1264 NSC 687852 (b-AP15) CAS:1009817-63-3 b-AP15 is a novel inhibitor of proteasome deubiquitination.b-AP15 displays antitumor activity in several preclinical,solid tumor models.b-AP15 triggers time-and dose-dependent apoptosis of the human multiple myeloma(MM)cell lines RPMI8226 and U266,as determined by phosphatidylserine exposure.b-AP15 may have potential for treatment of multiple myeloma patients. price>
R-R-2964 BI-3406 CAS No.2230836-55-0 BI-3406 (compound I-6)/CAS No.2230836-55-0 is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity. price>
R-C-1265 BIX 01294 CAS:1392399-03-9 BIX01294 is a potent chemical inhibitor of G9a methyltransferase that catalyzes the mono-and di-methylation of the lysine 9 residue of histone H3.BIX01294 suppresses osteoclast differentiation on mouse macrophage-like Raw264.7cells. BIX01294 enhances the cardiac potential of bone marrow cells. price>
R-R-2965 NSC 23766 trihydrochloride CAS No.1177865-17-6 NSC 23766 trihydrochloride/CAS No.1177865-17-6 is an inhibitor of Rac1 activation. price>
R-C-1266 LDN-57444 CAS:668467-91-2 LDN-57444 is a Uch-L1 inhibitor(ubiquitin C-terminal hydrolase-L1)with Ki=0.4 μ M.Ubiquitin carboxy-terminal hydrolase L1(UCH-L1)is an intracellular protein abundantly expressed in neurons,and a mutation in UCH-L1 has been identified in familial Parkinson is disease. price>