| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
IC50: 280 nM (METTL3)[1]
METTL3 (methyltransferase-like 3), the catalytic subunit of the N6-methyladenosine (m6A) methyltransferase complex. UZH1a inhibits METTL3 activity, thereby reducing m6A methylation levels on target RNAs. |
|---|---|
| ln Vitro |
UZH1a (2.5-160 μM; 72 h) suppresses the development of U2Os, HEK293T, and MOLM-13 cells with IC50 values of 11 μM, 67 μM, and 87 μM, respectively [1]. UZH1a (2.5–100 μM; 16 h) dose-dependently lowers the m6A methylation levels in MOLM-13 cell mRNA (IC50= 4.6 μM) [1]. UZH1a (40 μM; 16 hours) decreases the amounts of m6A methylation in the mRNA of MOLM-13, HEK293T, and U2Os cells [1]. MOLM-13 cells experience cell cycle arrest and increased apoptosis when exposed to UZH1a (20 μM) for 16 hours [1].
UZH1a suppresses the growth of U2Os, HEK293T, and MOLM-13 cells with IC₅0 values of 11 microM, 67 microM, and 87 microM, respectively. It dose-dependently lowers m6A methylation levels in MOLM-13 cell mRNA (IC₅0 = 4.6 microM). UZH1a (20 microM) induces cell cycle arrest and apoptosis in MOLM-13 cells. |
| ln Vivo |
No in vivo activity data has been reported for UZH1a in available literature. As a chemical probe for METTL3, it is primarily used in cell-based studies to investigate epitranscriptomic regulation.
|
| Enzyme Assay |
METTL3 inhibition assays: UZH1a is incubated with purified METTL3 enzyme and its substrate (RNA) in the presence of S-adenosylmethionine (SAM). Methyltransferase activity is measured by detecting the incorporation of methyl groups into RNA. IC₅0 values are calculated from dose-response curves.
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: MOLM-13, HEK293T, and U2Os cells Tested Concentrations: 2.5-160 µM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the growth of MOLM-13, HEK293T, and U2Os cells in a dose-dependent manner. m6A methylation levels are measured in MOLM-13, HEK293T, and U2Os cells treated with UZH1a using m6A RNA immunoprecipitation (MeRIP) or dot blot assays. Cell viability is assessed using MTT or CellTiter-Glo assays after 72 hours. |
| Animal Protocol |
No in vivo animal model data has been reported for UZH1a. As a METTL3 inhibitor chemical probe, it is primarily studied in vitro. Future studies could utilize xenograft models to evaluate its antitumor efficacy.
|
| ADME/Pharmacokinetics |
UZH1a has a molecular weight of 558.71 and a molecular formula of C32H42N₆O3. It is a selective METTL3 inhibitor with an IC₅0 of 280 nM. Detailed pharmacokinetic parameters have not been reported.
|
| Toxicity/Toxicokinetics |
No toxicity data has been published for UZH1a in mammalian systems. As a research compound and chemical probe, it is not intended for human therapeutic use. Cell-based assays indicate that UZH1a is tolerated at concentrations up to 160 microM in some cell lines.
|
| References | |
| Additional Infomation |
UZH1a is a potent and selective METTL3 inhibitor used as a chemical probe for studying epitranscriptomic regulation. By inhibiting METTL3, it reduces m6A methylation levels on target RNAs, affecting their stability, splicing, and translation. The compound is for research use only and has not entered clinical trials.
|
| Molecular Formula |
C32H42N6O3
|
|---|---|
| Molecular Weight |
558.714287281036
|
| Exact Mass |
558.331
|
| CAS # |
2813577-78-3
|
| Related CAS # |
UZH1;2925713-02-4;UZH1b;2814392-17-9
|
| PubChem CID |
154815692
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
4.8
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
9
|
| Heavy Atom Count |
41
|
| Complexity |
828
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC1(CCN(CC1)CC2=CC(=C(C=C2)C(=O)NC[C@@]3(CCCN(C3)C4=NC=NC(=C4)NCC5=CC=CC=C5)O)O)C
|
| InChi Key |
PWYRDVXYAOGDNK-JGCGQSQUSA-N
|
| InChi Code |
InChI=1S/C32H42N6O3/c1-31(2)12-15-37(16-13-31)20-25-9-10-26(27(39)17-25)30(40)34-21-32(41)11-6-14-38(22-32)29-18-28(35-23-36-29)33-19-24-7-4-3-5-8-24/h3-5,7-10,17-18,23,39,41H,6,11-16,19-22H2,1-2H3,(H,34,40)(H,33,35,36)/t32-/m1/s1
|
| Chemical Name |
N-[[(3R)-1-[6-(benzylamino)pyrimidin-4-yl]-3-hydroxypiperidin-3-yl]methyl]-4-[(4,4-dimethylpiperidin-1-yl)methyl]-2-hydroxybenzamide
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 80 mg/mL (143.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6 mg/mL (10.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 60.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 5.5 mg/mL (9.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 55.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.5 mg/mL (9.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7898 mL | 8.9492 mL | 17.8984 mL | |
| 5 mM | 0.3580 mL | 1.7898 mL | 3.5797 mL | |
| 10 mM | 0.1790 mL | 0.8949 mL | 1.7898 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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