About 33 results found for searched term "WS3" (0.086 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M11553 | WS3 | IκB/IKK |
| WS3 is a β cell proliferation inducer, which can promote the β cell proliferation of primary rat and human islets. WS3 can be used in the study of type I diabetes. | ||
| M29432 | WS-383 free base | E1/E2/E3 Enzyme |
| WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2. | ||
| M29433 | WS-383 | E1/E2/E3 Enzyme |
| WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2. | ||
| M30223 | WST-3 | Fluorescent Dye |
| WST-3 is a water-soluble tetrazolium dye. In the presence of an electron mediator, WST-3 is reduced to WST-3 formazan by NADH and displays an absorption maxima of 433 nM. | ||
| M1760 | Palomid 529 | mTOR |
| P529 | ||
| Palomid 529 (P529) is a novel potent PI3K/Akt/mTOR inhibitor and shows a potent antiproliferative activity in the NCI-60 cell lines panel, with growth inhibitory 50 (GI50) <35 μM. | ||
| M2304 | TWS119 | GSK-3 |
| TWS119 is a GSK-3β inhibitor with IC50 of 30 nM. | ||
| M2571 | GNF-2 | Src-bcr-Abl |
| GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. | ||
| M2913 | Palbociclib Isethionate | CDK |
| PD 0332991 isethionate | ||
| Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3. | ||
| M2982 | Ro 31-8220 Mesylate | PKC |
| Bisindolylmaleimide IX Mesylate | ||
| Ro 31-8220 is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively, and also shows potent inhibition against MAPKAP-K1b, MSK1, GSK3β and S6K1. | ||
| M3002 | Scriptaid | HDAC |
| Scriptide; GCK1026 | ||
| Scriptaid is an inhibitor of HDAC. It shows a greater effect on acetylated H4 than H3. | ||
| M6161 | GSK369796 Dihydrochloride | Potassium Channel |
| GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain. | ||
| M6168 | Ceritinib (LDK378) dihydrochloride | ALK |
| Ceritinib dihydrochloride | ||
| Ceritinib dihydrochloride (LDK378 dihydrochloride) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. | ||
| M6255 | JPH203 | Autophagy |
| KYT-0353 | ||
| JPH203, a selective L-type amino acid transporter 1 (LAT1) inhibitor, shows a dramatic inhibition of leucine uptake (IC50=0.06 µM) and cell growth (IC50=4.1 µM) in human colon cancer cells (HT-29), human oral cancer cells (YD-38) and leukemic cells. | ||
| M43838 | Almonertinib mesylate | EGFR/HER2 |
| HS-10296 mesylate | ||
| Almonertinib mesylate is an orally active, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR sensitization and T790M resistance mutations, and also shows strong inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37, 0.29, and 0.21 nM, respectively. The IC50 of T790M/Del19 was 0.37, 0.29 and 0.21 nM, respectively, but the inhibitory effect on wild-type was weaker, with an IC50 of 3.39 nM. It can be used in the research of non-small cell lung cancer. | ||
| M7437 | TWS 119 Trifluoroacetate | Others |
| TWS 119 Trifluoroacetate is a gSK-3β inhibitor; induces neuronal differentiation in ESCs. | ||
| M7509 | UNC0642 | Histone Methyltransferase |
| UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. | ||
| M8408 | CU-CPT22 | TLR |
| CU-CPT22 is the first probe for the complex between toll-like receptors TLR1 and TLR2. CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM. | ||
| M8529 | A-366 | Histone Methyltransferase |
| A366 | ||
| A-366 is a potent and highly selective peptide-competitive inhibitor of histone methyltransferase G9a, with IC50s of 3.3 nM and 38 nM for G9a and GLP, respectively, and is more than 1,000-fold selective for G9a and GLP over 21 other methyltransferases. A-366 is also a potent inhibitor of Spindlin1-H3K4me3 interaction (IC50=182.6 nM).A-366 shows high affinity for human H3R (Ki=17 nM) and exhibits subtype selectivity between subpopulations of the histaminergic and dopaminergic receptor families. It can be used for induction and maintenance of pluripotent stem cells in mice. | ||
| M9441 | GSK656 HCl | Anti-infection |
| GSK3036656; GSK070 hydrochloride | ||
| GSK656 is a potent Mtb LeuRS inhibitor, shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). | ||
| M10459 | MSA-2 | STING |
| MSA2 | ||
| MSA-2 is an orally available non-nucleotide STING agonist with antitumor activity. MSA-2 shows EC50 values of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. | ||
| M11127 | Sanggenol A | Others |
| Sanggenol A shows neuroprotective activity on glutamate-induced cell death in HT22 cells, with EC50 values of 34.03 ± 7.71 μM. Sanggenol A inhibits influenza A viral and pneumococcal neuraminidase (NA), it also disrupts the synergism between influenza A virus and pneumococcal NA in vitro, hence functioning as dual-acting anti-infectives. | ||
| M13624 | 6RK73 | Deubiquitinase |
| 6RK73 is a covalent irreversible and specific UCHL1 inhibitor with an IC50 of 0.23 µM. 6RK73 shows almost no inhibition of UCHL3 (IC50=236 µM). 6RK73 specifically inhibit UCHL1 activity in breast cancer. | ||
| M13660 | eIF4A3-IN-1 | Others |
| eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD. | ||
| M13736 | SIRT-IN-3 | Sirtuin |
| SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively). | ||
| M13770 | BCECF | Fluorescent Dye |
| 2′,7′-Bis(2-carboxyethyl)-5(6)-carboxyfluorescein | ||
| BCECF is a pH-sensitive fluorescent dye. BCECF allows measurements in the physiological pH range 6.0–8.0. Excitation ratio: 490/440 nm; Emission intensity: 535 nm. | ||
| M13854 | Lin28-let-7a antagonist 1 | Others |
| Lin28-let-7a antagonist 1 shows a clear antagonistic effect against the Lin28-let-7a interaction with an IC50 of 4.03 μM for Lin28A-let-7a-1 interaction. | ||
| M13927 | TAK-220 | CCR |
| TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA). | ||
| M14284 | Pico145 | TRP Channel |
| HC-608 | ||
| Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. | ||
| M14500 | Osoresnontrine | PDE |
| BI-409306 | ||
| Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders. | ||
| M14778 | Tafamidis meglumine | Transthyretin (TTR) |
| Fx-1006A | ||
| Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. | ||
| M19329 | Kuwanon T | Others |
| Kuwanon T is an isoprenylated flavonoid compound isolated from the root bark of Morus alba. Kuwanon T shows protective effects on t-BHP-induced oxidative stress with a EC50 of 30.32 μM. | ||
| M20644 | TH34 | HDAC |
| TH34 is a HDAC inhibitor that shows pronounced selectivity for HDACs 6, 8 and 10 over HDACs 1, 2 and 3. In a NanoBRET assay, TH34 strongly binds HDAC6, 8 and 10 with low-micromolar IC50 concentrations (HDAC6: 4.6 µM, HDAC8: 1.9 µM, HDAC10: 7.7 µM). | ||
| M20815 | WS-12 | TRP Channel |
| Acoltremon; AR-15512; AVX-012 | ||
| WS-12 (Acoltremon, AR-15512, AVX-012) is a potentially first-in-class, potent TRPM8 agonist with an EC50 of 39 nM. can be used in studies of dry eye and chronic neuropathic pain. | ||
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