TMX-4153
Based on 1 Customer Validation
TMX-4153 is a selective PIP4K2C PROTAC degrader. TMX-4153 induces PIP4K2C degradation in MOLT4 cells (DC50 = 24 nM) and HAP1 cells (DC50 = 361 nM). TMX-4153 can be used for the study of biological functions of PIP4K2C (immune modulation)-related diseases. (Pink: BTK ligand (HY-177432), Blue: VHL Ligand (HY-112078), Black: Linker).
(Pink: PIP4K2C ligand (HY-177432); Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.96%
- CAS No.: 2867519-91-1
- Formula: C59H67ClN10O6S
- Molecular Weight:1079.74
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Storage:Powder -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
All PROTACs Isoforms
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Biological Activity
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VHL |
PIP4K2C 61 nM (Kd) |
PIP4K2C 24 nM (DC50, MOLT4 cells) |
PIP4K2C 361 nM (DC50, HAP1 cells) |
TMX-4153 (0.01-1 μM, 2-24 h) induces PIP4K2C degradation in MOLT4 cells, with a DC50 of 24 nM[1].
TMX-4153 (0.01-5 μM, 6 h) exhibits moderate PIP4K2C degradation activity in HAP1 cells, with a DC50 of 361 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT4 cells
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Concentration:0.01, 0.05, 0.1, 0.5, 1 µM
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Incubation Time:6 h
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Result:Selectively degraded PIP4K2C with the maximal level of degradation (Dmax) value of 91% at 1 μM and half-maximal degradation concentration (DC50) value of 24 nM.
Chemical Information
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CAS No. 2867519-91-1
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Appearance Solid
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Molecular Weight 1079.74
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Formula C59H67ClN10O6S
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Color White to off-white
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SMILES
ClC1=CN=C(N=C1C2=CC=CC(C3=CC=CC=C3)=C2)NC4=CC(N(C5=O)CCC5(CC6)CCN6C(CCCCCC(N[C@H](C(N7[C@H](C(N[C@@H](C)C8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)C(C)(C)C)=O)=O)=CN=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (92.61 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. 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)
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 (2.32 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (2.32 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 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. 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 | 0.9261 mL | 4.6307 mL | 9.2615 mL | 23.1537 mL |
| 5 mM | 0.1852 mL | 0.9261 mL | 1.8523 mL | 4.6307 mL | |
| 10 mM | 0.0926 mL | 0.4631 mL | 0.9261 mL | 2.3154 mL | |
| 15 mM | 0.0617 mL | 0.3087 mL | 0.6174 mL | 1.5436 mL | |
| 20 mM | 0.0463 mL | 0.2315 mL | 0.4631 mL | 1.1577 mL | |
| 25 mM | 0.0370 mL | 0.1852 mL | 0.3705 mL | 0.9261 mL | |
| 30 mM | 0.0309 mL | 0.1544 mL | 0.3087 mL | 0.7718 mL | |
| 40 mM | 0.0232 mL | 0.1158 mL | 0.2315 mL | 0.5788 mL | |
| 50 mM | 0.0185 mL | 0.0926 mL | 0.1852 mL | 0.4631 mL | |
| 60 mM | 0.0154 mL | 0.0772 mL | 0.1544 mL | 0.3859 mL | |
| 80 mM | 0.0116 mL | 0.0579 mL | 0.1158 mL | 0.2894 mL |
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