PROTAC HDAC degrader-2 TFA
Based on 1 Customer Validation
PROTAC HDAC degrader-2 TFA is a selective class IIb dual histone deacetylase (HDAC6 and HDAC10) PROTAC degrader, with DC50 values of 13 nM and 29 nM against HDAC6 and HDAC10, respectively. It does not degrade class I (HDAC1/8) and class IIa (HDAC4/7) histone deacetylases.
(Pink: HDAC6 and HDAC10 ligand (HY-174471); Blue: Cereblon ligand (HY-131717); Black: linker).
For research use only. We do not sell to patients.
- Purity : 96.68%
- Formula: C42H44F3N7O9
- Molecular Weight:847.84
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
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hHDAC6 13 nM (DC50) |
hHDAC10 29 nM (DC50) |
In Vitro
PROTAC HDAC degrader-2 (AP1) TFA potently inhibits purified HDAC6 and HDAC10 enzymes with IC50 values of 0.040 μM and 0.022 μM, respectively[1].
PROTAC HDAC degrader-2 TFA engages cellular CRBN in HEK293T cells stably expressing NanoLuc-CRBN with an IC50 of 7.5 μM, an upper estimate due to autofluorescence interference[1].
PROTAC HDAC degrader-2 (50 nM, 1 μM; up to 1440 min) TFA shows high stability in human plasma at 1 μM, remaining above 85% intact for up to 1440 min[1].
PROTAC HDAC degrader-2 (1-5 μM; 24 h) TFA potently and selectively degrades HDAC6 and HDAC10 in MM.1S cells, with DC50 values of 13 nM and 29 nM, respectively, and no off-target degradation of class I or class IIa HDAC subtypes at 1 μM for 24 h[1].
PROTAC HDAC degrader-2 (1 μM; 24 h) TFA does not induce histone H3 hyperacetylation and shows minimal effects on acetylated α-tubulin in MM.1S cells treated with 1 μM for 24 h, confirming its class IIb HDAC selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:1 μM, 5 μM
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Incubation Time:24 h
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Result:Degraded 95% of HDAC6 and 93% of HDAC10 protein at 1 μM.
Degraded 96% of HDAC6 and 88% of HDAC10 protein at 5 μM.
Achieved a DC50 of 13 nM for HDAC6 degradation.
Achieved a DC50 of 29 nM for HDAC10 degradation.
Showed no degradation of HDAC1, HDAC4, HDAC7, or HDAC8.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Did not induce histone H3 hyperacetylation.
Showed minimal effects on acetylated α-tubulin compared to a pan-HDAC inhibitor control.
Chemical Information
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Appearance Solid
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Molecular Weight 847.84
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Formula C42H44F3N7O9
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Color Light yellow to yellow
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SMILES
O=C1CCC(C(N1)=O)N2C(C3=CC=CC(NCC(NCCCCCCN4CCC5=C(C6=CC=CC=C6N5CC7=CC=C(C=C7)C(NO)=O)C4)=O)=C3C2=O)=O.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (117.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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
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Data Sheet (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 | 1.1795 mL | 5.8973 mL | 11.7947 mL | 29.4867 mL |
| 5 mM | 0.2359 mL | 1.1795 mL | 2.3589 mL | 5.8973 mL | |
| 10 mM | 0.1179 mL | 0.5897 mL | 1.1795 mL | 2.9487 mL | |
| 15 mM | 0.0786 mL | 0.3932 mL | 0.7863 mL | 1.9658 mL | |
| 20 mM | 0.0590 mL | 0.2949 mL | 0.5897 mL | 1.4743 mL | |
| 25 mM | 0.0472 mL | 0.2359 mL | 0.4718 mL | 1.1795 mL | |
| 30 mM | 0.0393 mL | 0.1966 mL | 0.3932 mL | 0.9829 mL | |
| 40 mM | 0.0295 mL | 0.1474 mL | 0.2949 mL | 0.7372 mL | |
| 50 mM | 0.0236 mL | 0.1179 mL | 0.2359 mL | 0.5897 mL | |
| 60 mM | 0.0197 mL | 0.0983 mL | 0.1966 mL | 0.4914 mL | |
| 80 mM | 0.0147 mL | 0.0737 mL | 0.1474 mL | 0.3686 mL | |
| 100 mM | 0.0118 mL | 0.0590 mL | 0.1179 mL | 0.2949 mL |
PROTAC HDAC degrader-2 TFA Related Classifications
HY-174444A Related Classifications
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