ACHP

ACHP is an inhibitor of IkappaB kinase beta (IKKbeta) and IKKalpha (IC50s = 8.5 and 250 nM, respectively). It is selective for IKKbeta and IKKalpha over IKKgamma, Syk, and MKK4 (IC50s = >20 µM for all). It reduces the constitutive phosphorylation of IkappaBalpha and NF-kappaB p65 in U266 and NCU-MM-2 multiple myeloma cells when used at a concentration of 50 µM. ACHP (0.1 µM) prevents TNF-alpha-induced activation of NF-kappaB in U266 cells and inhibits the growth of U266, NCU-MM-2, and ILKM2 multiple myeloma and BJAB B cell lymphoma cells (IC50s = 18.3, 27.6, 34.6, and 17.6 µM, respectively). It prevents HIV-1 replication induced by TNF-alpha in OM10.1 cells latently infected with HIV-1 (EC50 = 0.56 µM). Topical administration of ACHP (5 mg/kg) prevents skin inflammation induced by phorbol 12-myristate 13-acetate (PMA, Cay-10008014) or imiquimod (Cay-14956) and reduces cytokine and chemokine expression induced by imiquimod in mice. It also prevents skin erythema induced by UV light and reduces the incidence of tumors induced by 7,12-dimethyl benzanthracene by 50% in mice when administered topically at a dose of 5 mg/kg.Formal Name: 2-amino-6-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-4-(4-piperidinyl)-3-pyridinecarbonitrile. CAS Number: 406208-42-2. Molecular Formula: C21H24N4O2. Formula Weight: 364.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 20 mM. SMILES: OC1=CC=CC(OCC2CC2)=C1C3=NC(N)=C(C#N)C(C4CCNCC4)=C3. InChi Code: InChI=1S/C21H24N4O2/c22-11-16-15(14-6-8-24-9-7-14)10-17(25-21(16)23)20-18(26)2-1-3-19(20)27-12-13-4-5-13/h1-3,10,13-14,24,26H,4-9,12H2,(H2,23,25). InChi Key: DYVFBWXIOCLHPP-UHFFFAOYSA-N.