DW-229
DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer.
(Pink: Histone Demethylase ligand (HY-B0568); Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- Formula: C38H41N5O7
- Molecular Weight:679.76
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
All PROTACs Isoforms
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Biological Activity
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Cereblon |
KDM2 |
KDM3 |
KDM4A |
KDM5B |
KDM6 |
DW-229 binds to purified E3 ligase and Fe2+/α-ketoglutarate-dependent KDMs (KDM6A, KDM5A, KDM5B, KDM3A, KDM2A)[1].
DW-229 (0.1-2.5 μM; 48 h) inhibits KDM activity in mES cells in a dose-dependent manner, with a transient heterochromatin-inducing effect at lower concentrations[1].
DW-229 (72 h) potently inhibits the proliferation of multiple cancer cell lines (A549, DU-145, LNCaP, HepG2, SK-HEP-1, MCF-7, MDA-MB-231, MDA-MB-453) with IC50 values ranging from < 0.5 μM to 8.87 μM, while showing minimal cytotoxicity against normal Vero cells[1].
DW-229 (0.5-8.0 μM; 24 h) significantly downregulates nuclear KDM5B and KDM6A expression in MCF-7 breast cancer cells[1].
DW-229 (2.5-40 μM; 24 h) exerts a biphasic effect on cytoplasmic KDM1A expression in MDA-MB-231 breast cancer cells[1].
DW-229 (0.9 μM; 24 h) downregulates the expression of multiple KDM genes in MCF-7 breast cancer cells, strongly reducing KDM2A, KDM3A, and KDM5B levels, and moderately reducing KDM4A-C, KDM5C, and KDM6B levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 breast cancer cells
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Concentration:0.5, 1.0, 2.0, 4.0, 8.0 μM
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Incubation Time:24 h
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Result:Significantly downregulated nuclear expression levels of KDM5B and KDM6A.
Had minimal effects on cytoplasmic and nuclear KDM1A, and cytoplasmic KDM6B.
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Cell Line:MDA-MB-231 breast cancer cells
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Concentration:2.5, 5, 10, 20, 40 μM
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Incubation Time:24 h
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Result:Exerted a biphasic effect on cytoplasmic KDM1A expression, with downregulation at lower concentrations and upregulation at higher concentrations.
Affected nuclear KDM1A expression only via upregulation at the highest concentration.
Exerted a nonsignificant biphasic effect on cytoplasmic KDM6B expression.
Showed no significant effect on nuclear KDM5B.
Chemical Information
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Molecular Weight 679.76
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Formula C38H41N5O7
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SMILES
O=C1N(C2C(NC(CC2)=O)=O)C(C3=CC=CC(NCCCCC#CC4=CC(C(NCCCCCCN5C(C)=C(O)C(C=C5)=O)=O)=CC=C4)=C31)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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