JPS014 TFA
Based on 1 Customer Validation
JPS014 TFA is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 TFA recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 TFA acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 TFA increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 TFA can be used for the research of colon cancer.
(Pink: HDAC1 and HDAC2 and HDAC3 ligand (HY-50934); Blue: VHL ligand (HY-125845); Black: linker).
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- Pureté: 98.12%
- Formule: C48H60F3N7O9S
- Masse moléculaire:968.09
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Stockage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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HDAC1 0.91 μM (DC50) |
HDAC2 4.19 μM (DC50) |
HDAC3 0.64 μM (DC50) |
VHL |
JPS014 (0.1-10 μM; 24-48 h) TFA induces submicromolar degradation of HDAC1 (DC50 = 0.91 μM), HDAC2 (DC50 = 4.19 μM), and HDAC3 (DC50 = 0.64 μM) in HCT116 cells, increases H3K56ac levels, reduces corepressor complex components SIN3A and LSD1, and exhibits a hook effect for HDAC3 at concentrations above 1 μM[1].
JPS014 (10 μM; 24-48 h) TFA reduces viability of HCT116 cells with an EC50 of 7.3 μM after 48 h and induces significant apoptosis, as measured by sub-G1 population, at 10 μM after 24 and 48 h[1].
JPS014 (10 μM; 24 h) TFA induces widespread transcriptional changes, with 3724 total DEGs, and enriches pathways linked to cell cycle regulation and apoptosis in HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:0.1, 1, 10 μM (24 h); 10 μM (48 h)
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Incubation Time:24 h (0.1, 1, 10 μM); 48 h (10 μM)
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Result:Induced degradation of HDAC1, HDAC2, and HDAC3 at 0.1, 1, and 10 μM for 24 h, with HDAC3 degradation significantly enhanced at 1 μM compared to PROTAC 1 (JPS004).
Increased H3K56ac levels to comparable or greater levels than HDAC inhibitor CI-994 and PROTAC 1.
Reduced SIN3A levels to 50% of control abundance after 24 h at 10 μM.
Significantly reduced LSD1 levels compared to DMSO and CI-994 controls after 48 h at 10 μM.
Exhibited a hook effect for HDAC3 at concentrations greater than 1 μM, where HDAC3 abundance increased rather than decreased, while HDAC1/2 levels continued to decrease.
Achieved degradation DC50 values of 0.91 μM for HDAC1, 4.19 μM for HDAC2, and 0.64 μM for HDAC3, with maximal degradation (Dmax) values of 74% for HDAC1, 56% for HDAC2, and 59% for HDAC3.
Showed submicromolar inhibitory activity against purified HDAC complexes, with IC50 values of 0.22 μM for HDAC1-CoREST, 0.36 μM for HDAC2-CoREST, and 0.14 μM for HDAC3-SMRT.
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Cell Line:HCT116 human colon carcinoma cells
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Concentration:10 μM
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Incubation Time:24 h ; 48 h
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Result:Caused a substantial percentage of cells to enter the sub-G1 phase, indicating significant apoptosis after 24 h at 10 μM.
Induced sub-G1 population levels comparable to PROTAC 1 and CI-994 after 48 h at 10 μM.
Reduced cell viability with an EC50 of 7.3 μM after 48 h.
Chemical Information
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Appearance Solid
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Masse moléculaire 968.09
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Formule C48H60F3N7O9S
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Color White to off-white
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SMILES
O=C(N[C@@H](C(C)(C)C)C(N1[C@H](C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)C[C@@H](O)C1)=O)CCCCCCCCOCC(NC4=CC=C(C(NC5=CC=CC=C5N)=O)C=C4)=O.OC(C(F)(F)F)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvant et solubilité
DMSO : 100 mg/mL (103.30 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, 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 (protect from light, 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (276 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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Instruction de manipulation (2659 KB)
Références
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, 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 |
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| DMSO | 1 mM | 1.0330 mL | 5.1648 mL | 10.3296 mL | 25.8240 mL |
| 5 mM | 0.2066 mL | 1.0330 mL | 2.0659 mL | 5.1648 mL | |
| 10 mM | 0.1033 mL | 0.5165 mL | 1.0330 mL | 2.5824 mL | |
| 15 mM | 0.0689 mL | 0.3443 mL | 0.6886 mL | 1.7216 mL | |
| 20 mM | 0.0516 mL | 0.2582 mL | 0.5165 mL | 1.2912 mL | |
| 25 mM | 0.0413 mL | 0.2066 mL | 0.4132 mL | 1.0330 mL | |
| 30 mM | 0.0344 mL | 0.1722 mL | 0.3443 mL | 0.8608 mL | |
| 40 mM | 0.0258 mL | 0.1291 mL | 0.2582 mL | 0.6456 mL | |
| 50 mM | 0.0207 mL | 0.1033 mL | 0.2066 mL | 0.5165 mL | |
| 60 mM | 0.0172 mL | 0.0861 mL | 0.1722 mL | 0.4304 mL | |
| 80 mM | 0.0129 mL | 0.0646 mL | 0.1291 mL | 0.3228 mL | |
| 100 mM | 0.0103 mL | 0.0516 mL | 0.1033 mL | 0.2582 mL |
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