ACHP

ACHP is an inhibitor of IκB kinase β (IKKβ) and IKKα (IC₅₀s = 8.5 and 250 nM, respectively).¹ It is selective for IKKβ and IKKα over IKKγ, Syk, and MKK4 (IC₅₀s = >20 µM for all). It reduces the constitutive phosphorylation of IκBα and NF-κB p65 in U266 and NCU-MM-2 multiple myeloma cells when used at a concentration of 50 µM.² ACHP (0.1 µM) prevents TNF-α-induced activation of NF-κB 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-α in OM10.1 cells latently infected with HIV-1 (EC₅₀ = 0.56 µM).³ Topical administration of ACHP (5 mg/kg) prevents skin inflammation induced by phorbol 12-myristate 13-acetate (PMA; Item No. 10008014) or imiquimod (Item No. 14956) and reduces cytokine and chemokine expression induced by imiquimod in mice.⁴ 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.

WARNING This product is not for human or veterinary use.

1. Murata, T., Shimada, M., Sakakibara, S., et al. Synthesis and structure-activity relationships of novel IKK-β inhibitors. Part 3: Orally active anti-inflammatory agents. Bioorg. Med. Chem. Lett. 14(15), 4019-4022 (2004).

2. Sanda, T., Iida, S., Ogura, H., et al. Growth inhibition of multiple myeloma cells by a novel Iκβ kinase inhibitor. Clin. Cancer Res. 11(5), 1974-1982 (2005).

3. Victoriano, A.F.B., Asamitsu, K., Hibi, Y., et al. Inhibition of human immunodeficiency virus type 1 replication in latently infected cells by a novel Iκβ kinase inhibitor. Antimicrob. Agents Chemother. 50(2), 547-555 (2006).

4. Li, L., Cataisson, C., Flowers, B., et al. Topical application of a dual ABC transporter substrate and NF-κB inhibitor blocks multiple sources of cutaneous inflammation in mouse skin. J. Invest. Dermatol. 139(7), 1506-1515 (2019).