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iHAP1 is an inhibitor of tubulin polymerization (IC50 = 0.87 µM in a cell-free assay) that was originally identified as an activator of a heterotrimeric protein phosphatase 2A (PP2A) complex containing the PP2A-B56epsilon regulatory B subunit in a study that has since been retracted. It does not bind to protein phosphatase 2 regulatory subunit 1A (PPP2R1A) when used at a concentration of 20 µM nor activate PP2A-B55alpha, PP2A-B56alpha, or PP2A-B56epsilon in a cell-free dephosphorylation assay at 10 µM. iHAP1 inhibits the proliferation of K562 leukemia cells (IC50 = 0.84 µM) and induces apoptosis in HeLa cells when used at a concentration of 0.5 µM. iHAP1 also inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 5.9 and 5.3 µM, respectively.Formal Name: (2-chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)-methanone. CAS Number: 105925-39-1. Synonyms: Improved Heterocyclic Activator of PP2A 1, Tubulin Inhibitor 6. Molecular Formula: C20H14ClNO2S. Formula Weight: 367.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml, DMSO: 1 mg/ml. SMILES: O=C(N1C2=C(SC3=CC=C(C=C31)Cl)C=CC=C2)C4=CC=C(C=C4)OC. InChi Code: InChI=1S/C20H14ClNO2S/c1-24-15-9-6-13(7-10-15)20(23)22-16-4-2-3-5-18(16)25-19-11-8-14(21)12-17(19)22/h2-12H,1H3. InChi Key: CSWHYHPUEDNIQY-UHFFFAOYSA-N.
Keywords:
Improved Heterocyclic Activator of PP2A 1, Tubulin Inhibitor 6, (2-chloro-10H-phenothiazin-10-yl)(4-methoxyphenyl)-methanone
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