Tubulin inhibitor 6

An inhibitor of tubulin polymerization and a PP2A activator

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5mg

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货号: ajcx16856
CAS: 105925-39-1
别名: Improved Heterocyclic Activator of PP2A 1, Tubulin Inhibitor 6
分子式: C20H14ClNO2S
分子量: 367.85
纯度: >98%
溶解度: DMSO: 62.5 mg/mL (169.91 mM)
储存: Store at -20°C
库存: 现货

Background

iHAP1 is an inhibitor of tubulin polymerization (IC₅₀ = 0.87 ?M) and an allosteric activator of a heterotrimeric protein phosphatase 2A (PP2A) complex containing the PP2A-B56ε regulatory B subunit.^1,2 It inhibits proliferation of K562 chronic myeloid leukemia (CML) cells (IC₅₀ = 0.84 ?M), induces cell cycle arrest at the G₂/M phase in KOPT-K1 T cell acute lymphoblastic leukemia (T-ALL) cells, and induces apoptosis in a variety of T-ALL cells (IC₅₀s = 0.4-0.6 ?M). iHAP1 reduces the frequency of human CD45⁺ leukemia cells in the bone marrow, spleen, and liver and increases survival in a KOPT-K1 mouse xenograft model when administered at doses of 2.5 and 80 mg/kg per day.²

1.Prinz, H., Chamasmani, B., Vogel, K., et al.N-benzoylated phenoxazines and phenothiazines: Synthesis, antiproliferative activity, and inhibition of tubulin polymerizationJ. Med. Chem.54(12)4247-4263(2011) 2.Morita, K., He, S., Nowak, R.P., et al.Allosteric activators of protein phosphatase 2A display broad antitumor activity mediated by dephosphorylation of MYBL2Cell181(3)702-715(2020)