PROTAC IRAK3 degrade-1 formic
Based on 1 Customer Validation
PROTAC IRAK3 degrader-1 formic is a potent and selective IRAK3 degrader with a DC50 of 0.002 μM. PROTAC IRAK3 degrader-1 formic induces proteasome-dependent degradation of IRAK3 via ternary complex formation with IRAK3 and CRBN. PROTAC IRAK3 degrader-1 formic can be used for cancer research.
(Pink: IRAK3 Target protein ligand; Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.26%
- Formula: C48H65N11O8
- Molecular Weight:924.10
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IRAK3[1]
PROTAC IRAK3 degrader-1 (compound 23) formic potently and selectively binds to recombinant IRAK3 with an IC50 of 5 nM, with 280-fold selectivity over IRAK4[1].
PROTAC IRAK3 degrader-1 formic binds to recombinant CRBN with an IC50 of 460 nM[1].
PROTAC IRAK3 degrader-1 formic shows primary selectivity for recombinant IRAK3 in a 400-kinase panel, with weaker inhibition of CDK11, CDK8, TRKC, and GSG2[1].
PROTAC IRAK3 degrader-1 formic selectively binds to IRAK3 in a chemoproteomic assay, with an apparent binding constant of 34 nM and >20-fold selectivity over all other detected targets[1].
PROTAC IRAK3 degrader-1 (0.0003-10 μM; 2-48 h) formic potently degrades IRAK3 in THP1 cells, sustained degradation[1].
PROTAC IRAK3 degrader-1 (0.1 μM; 8 h) formic selectively decreases IRAK3 protein levels in THP1 cells, with only minimal off-target effects on DHCR24 and no degradation of IKZF1, GSPT1, IRAK1, or IRAK4[1].
PROTAC IRAK3 degrader-1 (0.3 μM; 8-32 h) formic induces significant, sustained IRAK3 degradation in primary human macrophages, and this activity is unaffected by LPS stimulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP1 monocytic cancer cells
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Concentration:0.0003; 0.001; 0.003; 0.01; 0.03; 0.1; 0.3; 1; 3; 10 μM
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Incubation Time:2; 4; 6; 8; 16; 24; 48 h
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Result:Induced potent IRAK3 degradation with a DC50 of 2 nM and maximum degradation (Dmax) of 98% after 16 h.
Achieved maximal degradation at 0.1 μM after 24 h.
Detected degradation as early as 2 h after treatment with 0.1 μM, which persisted up to 48 h.
Allowed full IRAK3 recovery 24 h after compound washout.
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Cell Line:THP1 monocytic cancer cells
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Concentration:0.1; 0.3; 1; 3; 10 μM
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Incubation Time:6; 24 h
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Result:Fully rescued IRAK3 degradation when cells were pretreated with proteasome inhibitor MG132 or NEDD8-activating enzyme inhibitor MLN4924.
Prevented IRAK3 degradation when cells were pretreated with excess IRAK3 ligand 5 or thalidomide.
Chemical Information
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Appearance Solid
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Molecular Weight 924.10
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Formula C48H65N11O8
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Color Light yellow to yellow
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SMILES
O=C1C2=CC(N3CCN(CC3)CCC4CCN(CC4)C(CCC(N5CCN([C@@]6([H])CC[C@H](CC6)NC7=NC=NN8C7=C(C(C)C)C=C8)CC5)=O)=O)=CC=C2C(N1C9C(NC(CC9)=O)=O)=O.O=CO
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 150 mg/mL (162.32 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 and 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 (sealed storage, away from moisture and 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)
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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 5 mg/mL (5.41 mM); Clear solution; Need ultrasonic
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 (sealed storage, away from moisture and light)
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 (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 and 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 | 1.0821 mL | 5.4107 mL | 10.8213 mL | 27.0533 mL |
| 5 mM | 0.2164 mL | 1.0821 mL | 2.1643 mL | 5.4107 mL | |
| 10 mM | 0.1082 mL | 0.5411 mL | 1.0821 mL | 2.7053 mL | |
| 15 mM | 0.0721 mL | 0.3607 mL | 0.7214 mL | 1.8036 mL | |
| 20 mM | 0.0541 mL | 0.2705 mL | 0.5411 mL | 1.3527 mL | |
| 25 mM | 0.0433 mL | 0.2164 mL | 0.4329 mL | 1.0821 mL | |
| 30 mM | 0.0361 mL | 0.1804 mL | 0.3607 mL | 0.9018 mL | |
| 40 mM | 0.0271 mL | 0.1353 mL | 0.2705 mL | 0.6763 mL | |
| 50 mM | 0.0216 mL | 0.1082 mL | 0.2164 mL | 0.5411 mL | |
| 60 mM | 0.0180 mL | 0.0902 mL | 0.1804 mL | 0.4509 mL | |
| 80 mM | 0.0135 mL | 0.0676 mL | 0.1353 mL | 0.3382 mL | |
| 100 mM | 0.0108 mL | 0.0541 mL | 0.1082 mL | 0.2705 mL |
PROTAC IRAK3 degrade-1 formic Related Classifications
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