TO-1187 TFA
Based on 1 Customer Validation
TO-1187 TFA is a selective HDAC6 PROTAC degrader (DC50: 5.81 nM). TO-1187 TFA promotes the ubiquitination and degradation of HDAC6 and can be used in the study of hematological malignancies and solid tumors.
(Pink: HDAC6 ligand (HY-173386); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140212)).
For research use only. We do not sell to patients.
- Purity: 98.41%
- Formula: C36H36F3N9O9
- Molecular Weight:795.72
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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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
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HDAC6 5.81 nM (DC50) |
Cereblon |
TO-1187 (100 nM, 6 h) TFA highly selectively degrades HDAC6 in human multiple myeloma cells (MM.1S) (Dmax: 94%, DC50: 5.81 nM)[1].
TO-1187 (100 nM, 72 h) TFA does not show significant antiproliferative activity in MM.1S cells, indicating that it has low toxicity[1].
TO-1187 (1-10000 nM) TFA also exhibits a dose-dependent HDAC6 degradation ability in HeLa cells[1].
TO-1187 (100 nM, Pre-treatment for 1 h, then treatment for 6 h) TFA is degraded by CRBN E3 ligase and proteasome in MM.1S cells[1].
TO-1187 (100 nM, 6 h) TFA only degrades HDAC6 in MM.1S cells without affecting other proteins (such as CRBN novel substrates: IKZF1, IKZF3, CK1α, SALL4 and GSPT1), further confirming its high selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human multiple myeloma cells (MM.1S)
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Concentration:100 nM
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Incubation Time:0.5-24 h
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Result:Showed monoselectivity for HDAC6, and no degradation selectivity for other HDAC (such as HDAC3 and HDAC8) was observed at a concentration of 25 µM.
Initiated HDAC6 degradation within 30 minutes, the degradation rate reaches 45% within 1 hour, and the maximum degradation effect is achieved within 6 hours (Dmax: 94%).
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Cell Line:Human multiple myeloma cells (MM.1S)
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Concentration:100 nM
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Incubation Time:Pre-treatment for 1 h, then treatment for 6 h
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Result:Degraded HDAC6 via the ubiquitin-proteasome system mediates by CRBN E3 ligase, and its degradation can be competitively inhibited by proteasome inhibitors (MG132 (HY-13259) and Bortezomib (HY-10227)).
Dose-dependently blocked HDAC6 degradation by Thalidomide (HY-14658) (CRBN ligand), demonstrated its dependence on CRBN recruitment for degradation.
Chemical Information
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Appearance Solid
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Molecular Weight 795.72
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Formula C36H36F3N9O9
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=C(C=C1)CN(CC2=CN=CC=C2)CC3=CN(N=N3)CCOCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)NO.OC(C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (125.67 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (277 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 (stored under nitrogen). 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 | 1.2567 mL | 6.2836 mL | 12.5672 mL | 31.4181 mL |
| 5 mM | 0.2513 mL | 1.2567 mL | 2.5134 mL | 6.2836 mL | |
| 10 mM | 0.1257 mL | 0.6284 mL | 1.2567 mL | 3.1418 mL | |
| 15 mM | 0.0838 mL | 0.4189 mL | 0.8378 mL | 2.0945 mL | |
| 20 mM | 0.0628 mL | 0.3142 mL | 0.6284 mL | 1.5709 mL | |
| 25 mM | 0.0503 mL | 0.2513 mL | 0.5027 mL | 1.2567 mL | |
| 30 mM | 0.0419 mL | 0.2095 mL | 0.4189 mL | 1.0473 mL | |
| 40 mM | 0.0314 mL | 0.1571 mL | 0.3142 mL | 0.7855 mL | |
| 50 mM | 0.0251 mL | 0.1257 mL | 0.2513 mL | 0.6284 mL | |
| 60 mM | 0.0209 mL | 0.1047 mL | 0.2095 mL | 0.5236 mL | |
| 80 mM | 0.0157 mL | 0.0785 mL | 0.1571 mL | 0.3927 mL | |
| 100 mM | 0.0126 mL | 0.0628 mL | 0.1257 mL | 0.3142 mL |
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