PROTAC METTL3 degrader 1
Based on 1 Customer Validation
PROTAC METTL3 degrader 1 is a VHL-based PROTAC METTL3 degrader (DC50: 220 nM in MOLM-13 cells). PROTAC METTL3 degrader 1 inhibits METTL3/14 complex with an IC50 value of 341 nM. PROTAC METTL3 degrader 1 can be used for the research of acute myeloid leukemia and gastric cancer.
(Pink: METTL3 ligand (HY-115717); Blue: VHL ligand (HY-120217); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.14%
- Formula: C56H77F2N11O5S
- Molecular Weight:1054.34
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
Description
In Vitro
PROTAC METTL3 degrader 1 (KH12) inhibits the methyltransferase activity of the purified METTL3/METTL14 complex with an IC50 of 341 nM[1].
PROTAC METTL3 degrader 1 (KH12) (0.039-5 μM; 0-48 h) induces potent, dose- and time-dependent degradation of METTL3 in MOLM-13 cells, with a DC50 of 220 nM, 84% degradation at 1 μM for 24 h, and over 90% degradation at 1 μM for 24 h[1].
PROTAC METTL3 degrader 1 (KH12) (1 μM; 2.5 h pre-incubation, 6 h treatment) induces METTL3 degradation via the ubiquitin-proteasome system, not the autophagy-lysosomal pathway, in HEK293T cells[1].
PROTAC METTL3 degrader 1 (KH12) (72 h) potently suppresses the proliferation of MOLM-13 acute myeloid leukemia cells with an IC50 of 1.04 μM[1].
PROTAC METTL3 degrader 1 (KH12) (0.1-5 μM; 48 h) reduces c-MYC protein levels in a dose-dependent manner in MOLM-13 cells[1].
PROTAC METTL3 degrader 1 (KH12) (5 μM; 48 h) promotes myeloid differentiation of MOLM-13 acute myeloid leukemia cells, as demonstrated by increased CD11b expression[1].
PROTAC METTL3 degrader 1 (KH12) (1-10 μM; 48 h) induces dose-dependent apoptosis in MOLM-13 acute myeloid leukemia cells, with 78% apoptotic cells[1].
PROTAC METTL3 degrader 1 (KH12) (0.1-10 μM; 24 h) reduces METTL3 protein levels in GES-1 normal gastric cells, AGS gastric cancer cells, and SNU484 gastric cancer cells[1].
PROTAC METTL3 degrader 1 (KH12) (72 h) potently suppresses the proliferation of AGS and SNU484 gastric cancer cells with IC50 values of 1.48 μM and 3 μM respectively, while having minimal effect on GES-1 normal gastric cells[1].
PROTAC METTL3 degrader 1 (KH12) (1 μM; 24 h) reduces METTL3 protein levels in both cytoplasmic and nuclear fractions of AGS and SNU484 gastric cancer cells[1].
PROTAC METTL3 degrader 1 (KH12) (0.0001-100 μM; 5 days) significantly suppresses the growth of gastric cancer patient-derived organoids (GA215T and GA352T), with GA215T organoids showing greater sensitivity to the Target Reagent than to small molecule METTL3 inhibitors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HEK293T cells
-
Concentration:1 μM
-
Incubation Time:2.5 h (pre-incubation with inhibitors); 6 h (target reagent treatment)
-
Result:Induced METTL3 degradation.
Did not have its induced METTL3 degradation rescued by pre-treatment with 3-MA.
-
Cell Line:MOLM-13 cells
-
Concentration:0.1 μM, 1 μM, 5 μM
-
Incubation Time:48 h
-
Result:Reduced c-MYC protein levels in a dose-dependent manner.
-
Cell Line:MOLM-13 acute myeloid leukemia cells
-
Concentration:5 μM
-
Incubation Time:48 h
-
Result:Induced a significant increase in CD11b expression, indicating promotion of myeloid differentiation.
-
Cell Line:MOLM-13 acute myeloid leukemia cells
-
Concentration:1 μM, 5 μM, 10 μM
-
Incubation Time:48 h
-
Result:Induced apoptosis in a dose-dependent manner.
Induced 48% apoptotic cells at 5 μM.
Induced 78% apoptotic cells at 10 μM.
-
Cell Line:AGS gastric cancer cells, SNU484 gastric cancer cells
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Reduced METTL3 protein levels in both cytoplasmic and nuclear fractions of AGS and SNU484 cells.
Chemical Information
-
Appearance Solid
-
Molecular Weight 1054.34
-
Formula C56H77F2N11O5S
-
Color White to off-white
-
SMILES
O=C1NC2(CCN(C3=NC=NC(NCCCCCCCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)=C3)CC2)CN(C7=C(F)C=C(CN8CCC(C)(C)CC8)C(F)=C7)C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (94.85 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)
In Vivo:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (4.74 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
In Vivo Dissolution Calculator
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.
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 (275 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. 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 | 0.9485 mL | 4.7423 mL | 9.4846 mL | 23.7115 mL |
| 5 mM | 0.1897 mL | 0.9485 mL | 1.8969 mL | 4.7423 mL | |
| 10 mM | 0.0948 mL | 0.4742 mL | 0.9485 mL | 2.3712 mL | |
| 15 mM | 0.0632 mL | 0.3162 mL | 0.6323 mL | 1.5808 mL | |
| 20 mM | 0.0474 mL | 0.2371 mL | 0.4742 mL | 1.1856 mL | |
| 25 mM | 0.0379 mL | 0.1897 mL | 0.3794 mL | 0.9485 mL | |
| 30 mM | 0.0316 mL | 0.1581 mL | 0.3162 mL | 0.7904 mL | |
| 40 mM | 0.0237 mL | 0.1186 mL | 0.2371 mL | 0.5928 mL | |
| 50 mM | 0.0190 mL | 0.0948 mL | 0.1897 mL | 0.4742 mL | |
| 60 mM | 0.0158 mL | 0.0790 mL | 0.1581 mL | 0.3952 mL | |
| 80 mM | 0.0119 mL | 0.0593 mL | 0.1186 mL | 0.2964 mL |
PROTAC METTL3 degrader 1 Related Classifications
HY-162930 Related Classifications
Powered by Bioz