KL4-219A

SKU: orb2945990

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.

Research Area

Cell Biology

Key Properties

• MW: 370.47
• Purity: 99.68% (May vary between batches)
• Formula: C₂₀H₂₂N₂O₃S
• SMILES: O=C1[C@@]2(CN2[S@](C(C)(C)C)=O)C3=C(C=CC=C3)N1C4=CC=C(OC)C=C4
• Target: c-Myc

Bioactivity

• Target IC50:
  HDAC11:4.5 nM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KL4219A

Compound Identifiers

PubChem CID

176455487