Biological Activity
KL-1 is a small-molecule disruptor of the super elongation complex for transcriptional elongation and MYC-dependent cancer research. The compounds disrupted super elongation complex assembly and impaired release of promoter-paused RNA polymerase II.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| SEC disruption | AFF4–P-TEFb interaction study of KL-1 and KL-2. [1] | The compounds disrupted super elongation complex assembly and impaired release of promoter-paused RNA polymerase II. |
| Transcriptional consequence | Processive transcription and heat-shock-response assays. [1] | Reduced average elongation rate and attenuated heat-shock gene induction across the studied Drosophila and human systems. |
| MYC-associated response | Mammalian cellular transcriptional analyses. [1] | SEC inhibition lowered MYC and MYC-dependent transcriptional programs. |
In Vivo
No compound-specific animal efficacy result is established by the sources summarized here.
Compound and Evidence Context
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Animal attribution | The publication reports a MYC-driven mouse xenograft study. [1] | The verified abstract does not separate each KL-1/KL-2 dose and response. No compound-specific animal dose or inhibition percentage is assigned here. |
Interpretation
The study examines both KL-1 and KL-2. Shared abstract-level xenograft claims are not converted into compound-specific response rates.
