About 34 results found for searched term "50-14-6" (0.076 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M1677 | Afatinib | EGFR/HER2 |
| BIBW2992; Tomtovok; Tovok | ||
| Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. | ||
| M3278 | MK-5172 (Grazoprevir) | HCV Protease |
| Grazoprevir; MK5172 | ||
| MK-5172 is a novel NS3/4, a protease inhibitor for chronic HCV infection (Enzyme Ki for genotype1b, 2a, 2b and 3a at ＜0.02, 0.15, 0.02 and 0.7 nM, respectively). | ||
| M6056 | Vitamin D2 | DNA Methyltransferase |
| Ergocalciferol | ||
| Vitamin D2 is a selective inhibitor of mammalian DNA polymerase A (pol A) with IC50 of 123 mM. | ||
| M20318 | WAY-271127 | Others |
| WAY-271127 is a MtSk inhibitor. | ||
| M1817 | Y-27632 dihydrochloride | ROCK |
| Y27632; Y-27632 2HCl | ||
| Y-27632 is a potent, selective inhibitor of Rho-associated protein kinases (ROCK) with IC50 values of 140-220 nM for ROCK1 and ROCK2. In addition, Y-27632 inhibited LPA-induced entosis. | ||
| M2148 | RKI-1447 | ROCK |
| RKI-1447 is a potent small molecule inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 6 nM, respectively. | ||
| M2187 | ETP-46464 | ATM/ATR |
| ETP-46464 is a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα and ATM with IC50 of 0.6, 14, 36, 170 and 545 nM, respectively. | ||
| M2293 | CX-5461 | DNA/RNA Synthesis |
| Pidnarulex | ||
| CX-5461 (Pidnarulex) selectively inhibits Pol I-driven transcription of rRNA with IC50 of 142 nM in HCT-116 cells. | ||
| M2301 | NVP-TAE226 | FAK |
| TAE226 | ||
| Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. | ||
| M2824 | Lumiracoxib | COX |
| COX-189 | ||
| Lumiracoxib is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. | ||
| M2840 | Methazolamide | Carbonic Anhydrase |
| L584601 | ||
| Methazolamide is a carbonic anhydrase inhibitor with Ki of 50 nM, 14 nM and 36 nM for hCA I, hCA II and bCA IV isoforms, respectively. | ||
| M55629 | MIPS-21335 | PI3K |
| MIPS21335 | ||
| MIPS-21335 is a PI3KC2α inhibitor, with IC50 of 7 nM. MIPS-21335 also inhibits PI3KC2β, p110α, p110β and p110δ with IC50 values of 0.043, 0.140, 0.386, 0.742 μM, respectively. | ||
| 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. | ||
| M3486 | NPS-2143 | Calcium-sensing Receptor |
| SB262470 | ||
| NPS-2143 is a novel potent and selective antagonist of Ca(2+) receptor with IC50 of 43 nM. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca2+ concentrations (IC50=43 nM) elicited by activating the Ca2+ receptor in HEK 293 cells expressing the human Ca2+ receptor. | ||
| M3513 | GSK429286A | ROCK |
| RHO-15 | ||
| GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively. | ||
| M3578 | Amprenavir | HIV Protease |
| Amprenavir is an HIV protease inhibitor with IC50 of 14.6 ng/mL in wild-type HIV isolates. | ||
| M4058 | 11-oxo-mogroside-V | ROS |
| 11-Oxo-Mogroside V is a natural sweetener with strong antioxidant activity. 11-OXo-Mogroside V had a significant inhibitory effect on reactive oxygen species, and the EC50 of O2-, H2O2 and *OH were 4.79, 16.52 and 146.17 μg/mL, respectively. | ||
| M5335 | PF-4989216 | PI3K |
| PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. | ||
| M5472 | Butoconazole nitrate | Anti-infection |
| RS-35887 | ||
| Butoconazole (RS-35887) is an antifungal agent that inhibits phA-stimulated secretion of cytokines such as IL-2, TNFα, IFN and GM-CSF in human peripheral blood lymphocytes. IC50 were 7.2 μg/mL, 14.4 μg/mL, 7.36 μg/mL and 7.6 μg/mL, respectively. | ||
| M5863 | Pazopanib HCl (GW786034) | VEGFR/PDGFR |
| GW786034; Pazopanib Hydrochloride | ||
| Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. | ||
| M6362 | A 196 | Histone Methyltransferase |
| A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity. | ||
| M6649 | CZC-25146 | LRRK2 |
| CZC25146 | ||
| CZC 25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. | ||
| M6723 | Fenofibrate | PPAR |
| Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate inhibited cytochrome P450 subtype, with IC50 of 0.2, 0.7, 9.7, 4.8, and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively. | ||
| M7410 | THIP hydrochloride | GABA Receptor |
| Gaboxadol hydrochloride; Lu 02-030 HCl | ||
| THIP hydrochloride (Gaboxadol hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). | ||
| M10370 | Larazotide acetate | Others |
| AT-1001 | ||
| Larazotide acetate also known as AT-1001, is a tight junction regulator and reverses leaky junctions to their normally closed state. Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC50s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. | ||
| M10637 | GSK3368715 2HCl | PRMTs |
| EPZ019997 2HCl | ||
| GSK3368715 2HCl is a novel potent, orally active, reversible type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50 values of 3.1 nM, 48 nM, 1148 nM, 5.7 nM and 1.7 nM for PRMT1, PRMT3, PRMT4, PRMT6, PRMT8, respectively. | ||
| M10705 | NVP-2 | CDK |
| NVP-2 is an effective and selective ATP competitive cyclin-dependent kinase 9 (CDK9) probe that inhibits CDK9/CycT activity.IC50 The value is 0.514 nM. NVP-2 has inhibitory effects on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases, which IC50 The values are 0.584 μM, 0.706 μM, and 0.605 μM, respectively. NVP-2 induces apoptosis. | ||
| M10759 | GSK046 | Epigenetic Reader Domain |
| iBET-BD2 | ||
| GSK046 (iBET-BD2) is an effective, selective and orally active inhibitor of the BD2 bromine domain of the BET protein,IC50 The values are 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2), and 214 nM (BRDT BD2). GSK046 has immunomodulatory activity. | ||
| M11056 | NSC 617145 | DNA/RNA Synthesis |
| NSC 617145 is a selective werner syndrome helicase (WRN) helicase inhibitor,IC50 The value is 230 nM. NSC 617145 inhibit WRN ATPase and induce double-strand rupture (DSB) and chromosomal abnormalities. NSC 617145 is selective to WRN and superior to BLM, FANCJ, ChlR1, RecQ, and UvrD helicases. | ||
| M11405 | Inavolisib (GDC-0077) | PI3K |
| GDC-0077; RG6114；RO-7113755 | ||
| Inavolisib (GDC-0077; RG6114) is a potential best-in-class, orally selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutants compared to wild-type PI3Kα. It can trigger the degradation of mutation-producing PIK3α. | ||
| M13413 | JNJ-42226314 | MAGL |
| JNJ-42226314 is a competitive, highly selective and reversible inhibitor of non-covalent monoacylglycerol lipase (MAGL). The IC50s of JNJ-42226314 against human Hela cells, human PBMC, mouse brain and rat brain were 1.13 nM, 1.88 nM, 0.67 nM and 0.97 nM, respectively. | ||
| M13592 | ENMD-2076 Tartrate | Aurora Kinase |
| ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. | ||
| M13642 | CX-5461 dihydrochloride | DNA/RNA Synthesis |
| CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM). | ||
| M13713 | RK-287107 | PARP |
| RK-287107 is a potent and specific tankyrase inhibitor with IC50s of 14.3 and 10.6 nM for tankyrase-1 and tankyrase-2, respectively. RK-287107 blocks colorectal cancer cell growth. | ||
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