SEC inhibitor KL-2

• CAT Number: I018133
• CAS Number: 900308-51-2
• Molecular Formula: C17H13ClFNO3
• Molecular Weight: 333.74
• Purity: ≥95%
• Synonyms: (Z)-N-(5-chloro-2-methylphenyl)-4-(4-fluorophenyl)-4-hydroxy-2-oxobut-3-enamide
• InChI: InChI=1S/C17H13ClFNO3/c1-10-2-5-12(18)8-14(10)20-17(23)16(22)9-15(21)11-3-6-13(19)7-4-11/h2-9,21H,1H3,(H,20,23)/b15-9-
• InChIKey: FKGPCOZLGSAHRR-DHDCSXOGSA-N
• SMILES: CC1=C(C=C(C=C1)Cl)NC(=O)C(=O)C=C(C2=CC=C(C=C2)F)O

SEC inhibitor KL-2 (KL-2), a peptidomimetic lead compound, is a potent, selective super elongation complex (SEC) inhibitor and disrupts the interaction between the SEC scaffolding protein AFF4 and P-TEFb, resulting in impaired release of Pol II from promoter-proximal pause sites and a reduced average rate of processive transcription elongation. SEC inhibitor KL-2 exhibits an dose-dependent inhibitory effect on AFF4-CCNT1 interaction with a Ki of 1.50 μM[1].

Reference

[1]. Liang K, et al. Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced CancerTherapy. Cell. 2018 Oct 18;175(3):766-779.
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