PROTAC HDAC6 degrader 7 formic
Based on 1 Customer Validation
PROTAC HDAC6 degrader 7 formic is an orally active, highly efficient, and selective PROTAC degrader targeting histone deacetylase 6 (HDAC6) (IC50 = 118 nM). PROTAC HDAC6 degrader 7 formic can eliminate both the catalytic and zinc-finger ubiquitin-binding domain. PROTAC HDAC6 degrader 7 formic inhibits NLRP3 inflammasome assembly and activation, as well as blocks NF-κB signaling, thereby reducing the transcription and release of key inflammatory factors. PROTAC HDAC6 degrader 7 formic can reduce the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6. PROTAC HDAC6 degrader 7 formic can be used for the study of inflammatory bowel disease (IBD).
(Pink: HDAC6 ligand (HY-179422); Blue: Cereblon ligand (HY-W087383); Black: linker).
For research use only. We do not sell to patients.
- Formula: C50H56N8O8
- Molecular Weight:897.03
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
HDAC6 118 nM (IC50) |
NF-κB |
IL-6 |
NLRP3 |
Cereblon |
In Vitro
PROTAC HDAC6 degrader 7 (Compound 22f) (0-2 μM, 12 h) formic exhibits potent HDAC6 degradation activity in MV4-11 cells in a concentration-dependent manner (DC50 = 13.4 nM)[1].
PROTAC HDAC6 degrader 7 (25-200 nM, 12 h) formic shows only slight degradation of IKZF1 at 200 nM, but no degradation of GSPT1 in MV4-11 cells[1].
PROTAC HDAC6 degrader 7 (0-2 μM) formic demonstrates high specificity toward HDAC6 (IC50 of 118 nM) and exhibits no appreciable inhibition against other HDAC isotypes at 10 μM[1].
PROTAC HDAC6 degrader 7 (0.5 μM, 0-24 h) formic induces HDAC6 degradation in MV4-11 cells, which was initiated within 3 hours and reached equilibrium within 12 hours, and this degradation could be rescued by CRBN ligands and proteasome inhibitors, indicating that the mechanism of action is the induction of HDAC6 degradation via the CRBN-mediated ubiquitin-proteasome pathway[1].
PROTAC HDAC6 degrader 7 (0-6 μM, 0-24 h) formic degrades HDAC6 in J774A.1 cells in a time-dependent manner, with a concentration-dependent DC50 of 9.20 nM[1].
PROTAC HDAC6 degrader 7 (1.4-1000 nM, 8 h) formic significantly inhibits IL-1β in LPS (HY-D1056)/ATP-stimulated J774A.1 cells in a concentration-dependent manner[1].
PROTAC HDAC6 degrader 7 (40-200 nM, 8 h) formic significantly reduces the levels of mature IL-1β and p20 in J774A.1 cells at low concentrations, and downregulates the expression of intracellular NLRP3 and pro-IL-1β proteins at high concentrations[1].
PROTAC HDAC6 degrader 7 (0.2-1 μM) formic dose-dependently reduces the mRNA levels of NLRP3, pro-IL-1β, TNF-α, and IL-6 in LPS-induced J774A.1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 897.03
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Formula C50H56N8O8
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SMILES
O=CO.O=C(C1=CC=C(CN2C3=CC=CC=C3C=CC4=C2C=CC=C4OCCN5CCN(CC5)CC6CCN(C7=CC=C8C(C(N(C8=O)C9CCC(NC9=O)=O)=O)=C7)CC6)C=C1)NNCC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (111.48 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 (protect from light). 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 (protect from light). 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 (protect from light). 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 | 1.1148 mL | 5.5739 mL | 11.1479 mL | 27.8697 mL |
| 5 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL | 5.5739 mL | |
| 10 mM | 0.1115 mL | 0.5574 mL | 1.1148 mL | 2.7870 mL | |
| 15 mM | 0.0743 mL | 0.3716 mL | 0.7432 mL | 1.8580 mL | |
| 20 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3935 mL | |
| 25 mM | 0.0446 mL | 0.2230 mL | 0.4459 mL | 1.1148 mL | |
| 30 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9290 mL | |
| 40 mM | 0.0279 mL | 0.1393 mL | 0.2787 mL | 0.6967 mL | |
| 50 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5574 mL | |
| 60 mM | 0.0186 mL | 0.0929 mL | 0.1858 mL | 0.4645 mL | |
| 80 mM | 0.0139 mL | 0.0697 mL | 0.1393 mL | 0.3484 mL | |
| 100 mM | 0.0111 mL | 0.0557 mL | 0.1115 mL | 0.2787 mL |
PROTAC HDAC6 degrader 7 formic Related Classifications
HY-179421A Related Classifications
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