CAS NO. |
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1129403-56-0 |
Amcasertib |
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Amcasertib is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases |
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1496581-76-0 |
GNE-3511 |
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GNE-3511 is a potent and selective zipper kinase (DLK, MAP3K12) inhibitors. target: DLK, MAP3K12; IC50: 0.107 uM (DLK); In vitro: . The high dose of inhibitor GNE-3511 resulted in a completesuppression of c-Jun phosphorylation, while the low dose reduced the number of p-c-Jun positive cells to an intermediate level. protected primary neurons in an in vitro axon degeneration assay as well as reduced phosphorylation of the downstream transcription factor c-Jun. In vivo: GNE-3511 exhibites moderate (mouse, rat, and cynomolgus) to high (dog) in vivo plasma clearances, moderate volumes of distribution, short half-lives, and brain penetration sufficient to enable examination in animal models of neurodegeneration |
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1334719-95-7 |
Q203 |
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Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium. |
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1334719-95-7 |
Q203 |
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Q203 (IAP6) is a midazopyridine amide compound. Q203 is active against Mycobacterium tuberculosis H37Rv with an MIC50 of 2.7 nM in culture broth medium. |
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1037592-40-7 |
JPH203 |
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JPH203 is a potent and selective L-type amino acid transporter 1 inhibitor (LAT1), used for cancer research. |
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865305-30-2 |
AF-353 |
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AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist, inhibits human and rat P2X3 (pIC50= 8.0). IC50 value: pIC50 = 8.0 (pIC50, for P2X3) Target: P2X3/P2X2/3 receptor in vitro: AF-353 is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. AF-353 also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). [1] in vivo: SCI rats has significantly higher frequencies for field potentials and NVC than NL rats. Intravesical ATP increases field potential frequency in control but not SCI rats, while systemic AF-353 significantly reduces this parameter in both groups. AF-353 also reduces the inter-contractile interval in control but not in SCI rats; however, the frequency of NVC in SCI rats was significantly reduced.[2 |
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960293-88-3 |
BI605906 |
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BI605906, a novel inhibitor of IKKβ, inhibits IKKβ with an IC50 value of 380 nM when assayed at 0.1 mM ATP. IC50 value: 380 nM Target: IKKβ in vitro: BI605906 is a novel pharmacological inhibitors of the IKK family, inhibits IKKβ with an IC50 value of 380 nM when assayed at 0.1 mM ATP. The only other protein kinase that was inhibited of over 100 tested, which included IKKα and TBK1, was the IGF1 (insulin-like growth factor 1) receptor (IC50=7.6 μM). In IKKα?/? MEFs, BI605906 not only prevents the phosphorylation of physiological substrates, such as p105 and RelA, but also the phosphorylation of the serine residues in IKKβ (Ser177 and Ser181) that trigger its activation. |
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