PROTAC JAK1 degrader 1
Based on 1 Customer Validation
PROTAC JAK1 degrader 1 is a JAK1 PROTAC degrader with a DC50 of 214 nM and an IC50 of 5.2 nM. PROTAC JAK1 degrader 1 inhibits the downstream JAK-STAT signaling pathway by degrading JAK1. PROTAC JAK1 degrader 1 exhibits antiproliferative activity in cells. PROTAC JAK1 degrader 1 can be used for research on leukemia.
(Pink: JAK1 ligand (HY-10961); Blue: Cereblon ligand (HY-14658); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.97%
- CAS No.: 3052553-20-2
- Formula: C44H41N9O6
- Molecular Weight:791.85
-
Storage:
-20°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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
JAK1 214 nM (DC50) |
JAK1 5.2 nM (IC50) |
Cereblon |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEL | IC50 |
1.3 μM
Compound: 10c
|
Antiproliferative activity against HEL cells
Antiproliferative activity against HEL cells
|
[PMID: 38838918] |
| K562 | IC50 |
6.1 μM
Compound: 10c
|
Antiproliferative activity against human K562 cells
Antiproliferative activity against human K562 cells
|
[PMID: 38838918] |
| THP-1 | IC50 |
10.5 μM
Compound: 10c
|
Antiproliferative activity against human THP-1 cells
Antiproliferative activity against human THP-1 cells
|
[PMID: 38838918] |
PROTAC JAK1 degrader 1 (Compound 10c) (0.12-10 μM; 0-24 h) selectively degrades JAK1 in Hel cells in a time- and concentration-dependent, proteasome-dependent manner with a DC50 of 214 nM, while sparing JAK2, JAK3, and TYK2, and suppresses downstream JAK-STAT signaling via JAK1 degradation[1].
PROTAC JAK1 degrader 1 potently inhibits proliferation of Hel, THP-1, and K562 cells with IC50 values of 1.3 nM, 6.1 nM, and 10.5 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human erythroleukemia (Hel) cells
-
Concentration:0.12, 0.36, 1.1, 3.3 and 10 μM
-
Incubation Time:0, 1, 3, 8, 12 and 24 h
-
Result:Induced 79.5% degradation of JAK1 and only 16.0% degradation of JAK2 at 10 μM for 24 h.
Induced > 70% JAK1 degradation within 8 h at 5 μM, with time-dependent degradation observed through 24 h.
Induced concentration-dependent JAK1 degradation with a DC50 of 214 nM, and failed to induce significant degradation of JAK2, JAK3, or TYK2 at tested concentrations.
Blocked JAK1 degradation was observed when cells were pretreated with MG132 (10 μM), MLN4924 (100 nM), or carfilzomib (100 nM) prior to 5 μM compound treatment for 24 h.
Induced JAK1 degradation and suppressed phosphorylation of STAT1 and STAT3 at 1 μM for 24 h; this suppression was attenuated by co-treatment with MG132 (10 μM).
Chemical Information
-
CAS No. 3052553-20-2
-
Appearance Solid
-
Molecular Weight 791.85
-
Formula C44H41N9O6
-
Color Yellow to brown
-
SMILES
O=C(NCC#N)C1=CC=C(C2=NC(NC3=CC=C(N4CCC(C(NCCCCC#CC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)=O)CC4)C=C3)=NC=C2)C=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (126.29 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 (3.16 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (274 KB)
-
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)
-
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 (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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.2629 mL | 6.3143 mL | 12.6287 mL | 31.5716 mL |
| 5 mM | 0.2526 mL | 1.2629 mL | 2.5257 mL | 6.3143 mL | |
| 10 mM | 0.1263 mL | 0.6314 mL | 1.2629 mL | 3.1572 mL | |
| 15 mM | 0.0842 mL | 0.4210 mL | 0.8419 mL | 2.1048 mL | |
| 20 mM | 0.0631 mL | 0.3157 mL | 0.6314 mL | 1.5786 mL | |
| 25 mM | 0.0505 mL | 0.2526 mL | 0.5051 mL | 1.2629 mL | |
| 30 mM | 0.0421 mL | 0.2105 mL | 0.4210 mL | 1.0524 mL | |
| 40 mM | 0.0316 mL | 0.1579 mL | 0.3157 mL | 0.7893 mL | |
| 50 mM | 0.0253 mL | 0.1263 mL | 0.2526 mL | 0.6314 mL | |
| 60 mM | 0.0210 mL | 0.1052 mL | 0.2105 mL | 0.5262 mL | |
| 80 mM | 0.0158 mL | 0.0789 mL | 0.1579 mL | 0.3946 mL | |
| 100 mM | 0.0126 mL | 0.0631 mL | 0.1263 mL | 0.3157 mL |
PROTAC JAK1 degrader 1 Related Classifications
HY-162608 Related Classifications
Powered by Bioz