ZS3-046
ZS3-046 is a potent TAF1 PROTAC degrader with a DC50 < 10 nM. ZS3-046 recruits the CRBN E3 ubiquitin ligase, promotes polyubiquitination and proteasomal degradation of TAF1, thereby activating p53 and downregulating c-Myc, and ultimately induces apoptosis of tumor cells. ZS3-046 can be used in research related to acute myeloid leukemia.
(Pink: TAF1 ligand (HY-176467); Blue: Cereblon ligand (HY-41547); Black: linker (HY-176469)).
For research use only. We do not sell to patients.
- CAS No.: 3087879-97-5
- Formula: C49H57N9O7
- Molecular Weight:884.03
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TAF1 < 10 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MOLM-13 | DC50 |
< 10 nM
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Half-maximal degradation of TAF1 in unspecified cancer cell lines.
Half-maximal degradation of TAF1 in unspecified cancer cell lines.
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40376796 |
ZS3-046 (< 10 nM) potently induces TAF1 degradation in cancer cell lines with a DC50 < 10 nM[1].
ZS3-046 (100 nM; 8 h) treatment of Molm13 AML cells alters expression of 4380 genes, including p53 targets, reflecting TAF1's role in transcription initiation and complex regulation of p53 activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Molm13 cell
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Concentration:2, 10, 50, 250 nM
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Incubation Time:18 h
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Result:Potently degraded TAF1 protein in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Athymic Nude-Foxn1nu (female, 6-week old, subcutaneously injected with HL60 cells to induce acute myeloid leukemia)[1]
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Dosage:5, 10 mg/kg
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Administration:i.p.; once every 4-5 days; 4 total injections; for 14 days
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Result:Tumor growth was significantly inhibited following treatment with doses of 5 mg/kg and 10 mg/kg.
No significant weight loss was observed throughout the dosing and observation periods, indicating good tolerability and an absence of apparent toxicity.
Chemical Information
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CAS No. 3087879-97-5
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Molecular Weight 884.03
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Formula C49H57N9O7
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SMILES
O=C(N1C2CCC(NC2=O)=O)C3=C(NCC4CCN(CCCCCCCN5C6=C(C(C(C7=C8NC=C7)=CN(CCC=C)C8=O)=CC(C(N9CCOCC9)=O)=C6)N=C5)CC4)C=CC=C3C1=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)
ZS3-046 Related Classifications
HY-176457 Related Classifications
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