PS-1145

• CAT Number: I003539
• CAS Number: 431898-65-6
• Molecular Formula: C₁₇H₁₁ClN₄O
• Molecular Weight: 322.75
• Purity: ≥95%
• Target: IκB/IKK
• Solubility: DMSO: ≥ 43 mg/mL
• Storage: 2-8°C
• IC50: 88 nM [1]
• IUPAC Name: N-(6-chloro-9H-pyrido[3,4-b]indol-8-yl)pyridine-3-carboxamide
• InChI: InChI=1S/C17H11ClN4O/c18-11-6-13-12-3-5-20-9-15(12)21-16(13)14(7-11)22-17(23)10-2-1-4-19-8-10/h1-9,21H,(H,22,23)
• InChIKey: JZRMBDHPALEPDM-UHFFFAOYSA-N
• SMILES: C1=CC(=CN=C1)C(=O)NC2=CC(=CC3=C2NC4=C3C=CN=C4)Cl

PS-1145（Cat No.:I003539） is a highly specific inhibitor of IKK (IκB kinase), with an IC50 value of 88 nM. By selectively targeting IKK, an enzyme involved in the activation of NF-κB (nuclear factor kappa-light-chain-enhancer of activated B cells), PS-1145 effectively suppresses the NF-κB signaling pathway. This inhibition can modulate inflammatory responses and potentially hinder the progression of diseases associated with aberrant NF-κB activation, such as autoimmune disorders and certain cancers.

Reference

[1]. Hideshima T, et al. NF-kappa B as a therapeutic target in multiple myeloma. J Biol Chem. 2002 May 10;277(19):16639-47.
[2]. Cho J, et al. Tpl2 (tumor progression locus 2) phosphorylation at Thr290 is induced by lipopolysaccharide via an Ikappa-B Kinase-beta-dependent pathway and is required for Tpl2 activation by external signals. J Biol Chem. 2005 May 27;280(21):20442-8.
[3]. Gasparian AV, et al. Targeting transcription factor NFkappaB: comparative analysis of proteasome and IKK inhibitors. Cell Cycle. 2009 May 15;8(10):1559-66.
[4]. Cilloni D, et al. The NF-kappaB pathway blockade by the IKK inhibitor PS1145 can overcome imatinib resistance. Leukemia. 2006 Jan;20(1):61-7.
[5]. Shukla S, et al. Apigenin blocks IKKα activation and suppresses prostate cancer progression. Oncotarget. 2015 Oct 13;6(31):31216-32.