UNC6535 TFA
Based on 1 Customer Validation
UNC6535 TFA is a covalent ligand targeting the triple Tudor domain (3TD) of SETDB1. UNC6535 TFA reversibly binds to the aromatic cages of both TD2 and TD3 within SETDB1 3TD simultaneously, weakly inhibits the methyltransferase activity of SETDB1, and displaces the H3K9Me2K14Ac peptide from SETDB1 3TD.
For research use only. We do not sell to patients.
- Formula: C29H46F6N6O6
- Molecular Weight:688.70
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
UNC6535 TFA reversibly binds to the purified tripartite Tudor domain of SETDB1 and displaces the H3K9Me2K14Ac peptide, with an IC50 of 3.4 μM[1].
UNC6535 TFA binds to the purified triple Tudor domain of SETDB1, with a measured Kd of 4.2 μM determined by isothermal titration calorimetry[1].
UNC6535 TFA inhibits the methyltransferase activity of purified full-length SETDB1 protein, with an IC50 of 84 μM[1].
UNC6535 TFA inhibits the methyltransferase activity of purified truncated SETDB1-S (lacking the triple Tudor domain) with an IC50 of 30 μM[1].
UNC6535 TFA displaces the H3K9Me2K14Ac peptide from purified truncated SETDB1-S (lacking the tripartite Tudor domain) via fluorescence polarization, with an IC50 of 8.6 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Oil
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Molecular Weight 688.70
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Formula C29H46F6N6O6
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SMILES
COC1=CC2=C(C(NCCCCCCN(C)C)=NC(NCCCCCN(C)C)=N2)C=C1OC.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (145.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4520 mL | 7.2601 mL | 14.5201 mL | 36.3003 mL |
| 5 mM | 0.2904 mL | 1.4520 mL | 2.9040 mL | 7.2601 mL | |
| 10 mM | 0.1452 mL | 0.7260 mL | 1.4520 mL | 3.6300 mL | |
| 15 mM | 0.0968 mL | 0.4840 mL | 0.9680 mL | 2.4200 mL | |
| 20 mM | 0.0726 mL | 0.3630 mL | 0.7260 mL | 1.8150 mL | |
| 25 mM | 0.0581 mL | 0.2904 mL | 0.5808 mL | 1.4520 mL | |
| 30 mM | 0.0484 mL | 0.2420 mL | 0.4840 mL | 1.2100 mL | |
| 40 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9075 mL | |
| 50 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7260 mL | |
| 60 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6050 mL | |
| 80 mM | 0.0182 mL | 0.0908 mL | 0.1815 mL | 0.4538 mL | |
| 100 mM | 0.0145 mL | 0.0726 mL | 0.1452 mL | 0.3630 mL |
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