CAS NO. |
Products Name |
504433-23-2 |
GW 441756 |
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GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2. IC50 Value: 2 nM [1] Target: TrkA in vitro: GW441756 specifically blocked TrkA-induced cell death in a dose-dependent manner, but there was no effect in uninduced cells. TrkA ability to induce γH2AX production was significantly downregulated by both K-252a and GW441756 in the absence of DNA damage inducer. In addition, it was also suppressed by K-252a during DNA damage by doxorubicin treatment, but not by GW441756 |
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83797-69-7 |
6-OAU |
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6-OAU(GTPL5846; 6-n-octylaminouracil) is a surrogate agonist of GPR84; activates human GPR84 in the presence of Gqi5 chimera in HEK293 cells with an EC50 of 105 nM in the PI assay. IC50 value: 105 nM [1] Target: GPR84 agonist in vitro: 6-OAU increased [35S]GTPγS incorporated in Sf9 cell membranes expressing human GPR84-Gαi fusion protein with an EC50 of 512 nM. 6-OAU did not activate human GPR40 in HEK293 cells in the PI assay. Stimulation with 6.25 μm 6-OAU began to induce GPR84-EGFP internalization, and the extensive internalization was observed at 200 μm 6-OAU stimulation. In a Transwell assay, 3-OH-C12 and the surrogate agonist, 6-OAU, provoked chemotaxis of PMNs prepared from human peripheral blood in a concentration-dependent manner with an EC50 of 24.2 μm and 318 nm, respectively. In addition, 3-OH-C12 and 6-OAU increased the secretion of IL-8 from LPS-stimulated PMNs [1]. in vivo: Injection of 6-OAU suspension in 1% rat serum into the rat jugular vein (10 mg/kg) leads to the elevation of a chemokine, CXCL1 concentration in the serum peaking at 3 h after the injection. In the rat air pouch model, 6-OAU at 1 mg/ml dissolved in 0.3% BSA attracted both PMNs and macrophages into the air pouch, peaking at 4 h after 6-OAU inoculation |
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1449779-49-0 |
DGAT1-IN-1 |
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DGAT1-IN-1 is a potent DGAT1 inhibitor with IC50 of < 10 nM(cell lysate from Hep3B cells overexpressing human DGAT1). IC50 value: < 10 nM Target: DGAT1 inhibitor Imidazopyridine and imidazothiazole compounds as inhibitors of diacylglycerol o-acyltransferase type 1 enzyme and their preparation By Kim, Dooseop; Bok, Juhan; Shin, Sunmi From PCT Int. Appl. (2013), WO 2013119040 A1 20130815. |
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2227425-05-8 |
PF-06869206 |
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PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM. |
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LOXO195 |
LOXO195 |
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Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor (TKI), with IC50s of 0.6 nM, <2.5 nM for TRKA and TRKC respectively. |
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284028-89-3 |
XAV939 |
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XAV-939 is a Wnt/β-catenin pathway inhibitor. XAV-939 stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 and tankyrase 2 (IC50s of 5 and 2 nM,respectively), thereby stimulating β-catenin degradation. XAV939 binds tightly to the catalytic (PARP) domains of TNKS1 and TNKS2 (Kds of 99 and 93 nM, respectively) |
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1379686-30-2 |
SR9009 |
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SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively. |
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917389-32-3 |
Letermovir |
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Letermovir is a novel inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors. |
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144875-48-9 |
Resiquimod |
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Resiquimod is a Toll-like receptor 7 and 8 (TLR7/TLR8) agonist that induces the upregulation of cytokines such as TNF-α, IL-6 and IFN-α. |
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