| Identification | Back Directory | [Name]
SEC inhibitor KL-2 | [CAS]
900308-51-2 | [Synonyms]
KL2;KL-2;KL 2
2-Butenamide, N-(5-chloro-2-methylphenyl)-4-(4-fluorophenyl)-2-hydroxy-4-oxo- | [Molecular Formula]
C17H13ClFNO3 | [MDL Number]
MFCD14741815 | [MOL File]
900308-51-2.mol | [Molecular Weight]
333.74 |
| Chemical Properties | Back Directory | [Boiling point ]
521.1±50.0 °C(Predicted) | [density ]
1.400±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
8.09±0.50(Predicted) | [color ]
Light yellow to yellow | [SMILES]
CC1=CC=C(Cl)C=C1NC(/C(O)=C/C(C2=CC=C(F)C=C2)=O)=O |
| Hazard Information | Back Directory | [Uses]
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]. | [Biochem/physiol Actions]
Disruptor of SEC (super elongation complex) | [in vivo]
SEC inhibitor KL-2 (10 mg/kg, i.p., once daily for 15 days) delays tumor growth and prolonged survival in the MDA231-LM2 xenograft tumor model in nude mice[1]. | Animal Model: | MDA231-LM2 xenograft tumor model in nude mice[1] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection (i.p.), once daily for 15 days | | Result: | Significantly delayed tumor growth and increased survival of mice. |
| [References]
[1] Liang K, et al. Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced CancerTherapy. Cell. 2018 Oct 18;175(3):766-779. DOI:10.1016/j.cell.2018.09.027 |
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| Company Name: |
Merck KGaA
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21-20338288 |
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www.sigmaaldrich.cn |
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Biorbyt Ltd.
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+44 (0)1223 859 353 |
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http://www.biorbyt.com |
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