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KL4-219A is a selective covalent degrader of the oncogenic transcription factor MYC, inhibiting MYC transcriptional activity and degrading MYC in a proteasome-dependent manner by targeting intrinsically disordered C203 and D205 residues.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $164 | In Stock | |
5 mg | $361 | In Stock | |
10 mg | $539 | In Stock | |
25 mg | $996 | In Stock | |
50 mg | $1,597 | In Stock | |
100 mg | $2,556 | In Stock |
Description | KL4-219A is a selective covalent degrader of the oncogenic transcription factor MYC, inhibiting MYC transcriptional activity and degrading MYC in a proteasome-dependent manner by targeting intrinsically disordered C203 and D205 residues. |
Targets&IC50 | HDAC11:4.5 nM |
In vitro | KL4-219A potently inhibits HDAC11 in human cancer cell lines such as MDA-MB-231 and HCT116, with an IC₅₀ of 4.5 nM. KL4-219A increases H3K9 acetylation levels and boosts IL-10 expression in vitro. KL4-219A also suppresses MYC expression in immune cells and modulates pathways related to inflammation and metabolism[1]. |
In vivo | In C57BL/6J mice, KL4-219A was administered intraperitoneally at 50 mg/kg daily for 14 days, resulting in marked downregulation of MYC and upregulation of IL-10 in tumor tissue. In a breast cancer xenograft model, KL4-219A significantly reduced tumor volume compared to vehicle controls, with no observed toxicity[1]. |
Alias | KL4219A |
Molecular Weight | 356.48 |
Formula | C20H24N2O2S |
Smiles | COC(C=C1)=CC=C1N2C3=CC=CC=C3[C@@]4(N([S@](C(C)(C)C)=O)C4)C2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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