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SEC inhibitor KL-1

Chemical Structure : SEC inhibitor KL-1

CAS No.: 900308-84-1

SEC inhibitor KL-1

Catalog No.: PC-35724Not For Human Use, Lab Use Only.

SEC inhibitor KL-1 is a peptidomimetic inhibitor of super elongation complex (SEC) and transcription elongation by Pol II, disrupts cyclin T1-AFF4 interaction (Ki=3.48 uM) within SEC.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SEC inhibitor KL-1 is a peptidomimetic inhibitor of super elongation complex (SEC) and transcription elongation by Pol II, disrupts cyclin T1-AFF4 interaction (Ki=3.48 uM) within SEC。
SEC inhibitor KL-1 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-1 attenuates the heat-shock response from Drosophila to human, reduces protein levels of SEC components AFF1 and AFF4, but not CDK9 or CCNT1 in HEK293T cells.
SEC inhibitor KL-1 downregulates MYC and MYC-dependent transcriptional programs in mammalian cells and delays tumor progression in mouse xenograft models of MYC-driven cancer.

Physicochemical Properties

M.Wt 345.779
Formula C18H16ClNO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-chloro-2-methylphenyl)-4-(3-methoxyphenyl)-2,4-dioxobutanamide

References

1. Liang K, et al. Cell. 2018 Oct 18;175(3):766-779.e17.

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