| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
UZH1 targets METTL3 (methyltransferase-like 3), a key component of the N6-methyladenosine (m6A) methyltransferase complex. UZH1a is a potent and specific METTL3 inhibitor. The compound serves as a chemical probe for studying METTL3 function in RNA metabolism and gene expression.
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| ln Vitro |
UZH1 a (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]. MOLM-13, HEK293T, and U2Os cells are inhibited in growth by UZH1 b (2.5-160 μM; 72 h), with IC50 values of 78 μM, 79 μM, and 93 μM [1]. In MOLM-13 cells, UZH1 b is less active at concentrations up to 100 μM, while UZH1 a (2.5-100 μM; 16 hours) decreases m6A methylation levels in cellular mRNA in a dose-dependent manner (IC50=4.6 μM). Low [1]. The m6A methylation levels in MOLM-13, HEK293T, and U2Os cell mRNA are decreased by UZH1 a (40 μM; 16 h) [1]. In MOLM-13 cells, UZH1a (20 μM; 16 hours) promotes apoptosis and induces cell cycle arrest [1].
UZH1a inhibits METTL3 with an IC50 of 280 nM, while UZH1b (IC50 = 28 μM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. The compound has antitumor activity. |
| ln Vivo |
UZH1 has antitumor activity. In vivo activity data are limited but the compound shows promise as a chemical probe for studying METTL3 function in cancer biology and developmental processes. Further in vivo studies are needed.
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| Enzyme Assay |
In vitro enzyme assays measure METTL3 inhibition using recombinant METTL3 enzyme or methyltransferase assays. IC50 values are determined by assessing methyltransferase activity in the presence of varying concentrations of UZH1a.
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| Cell Assay |
Cell-based assays measure the effects of UZH1 on m6A RNA modification levels, gene expression, and cellular processes. Antitumor activity is assessed in cancer cell lines. The compound's ability to modulate epitranscriptomic regulation is evaluated.
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| Animal Protocol |
In vivo efficacy is evaluated in xenograft models of METTL3-dependent cancers. The compound's ability to inhibit tumor growth through METTL3 inhibition is assessed. Further studies are needed to fully characterize its in vivo antitumor activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for UZH1 are limited. As a small molecule METTL3 inhibitor, it may have favorable oral bioavailability. Further pharmacokinetic studies are needed to determine its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for UZH1 are limited. As a METTL3 inhibitor, it may have on-target effects related to m6A RNA modification. Standard laboratory safety precautions should be followed. Further toxicological studies are needed for comprehensive safety assessment.
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| References | |
| Additional Infomation |
UZH1 is the racemate of UZH1a and UZH1b. UZH1a is a potent and specific METTL3 inhibitor with an IC50 of 280 nM. UZH1 can be used for epitranscriptomic modulation of cellular processes and has antitumor activity. It serves as a valuable chemical probe for studying METTL3 function in cancer biology and developmental processes.
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| CAS # |
2925713-02-4
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| Related CAS # |
UZH1a;2813577-78-3;UZH1b;2814392-17-9
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| Appearance |
Off-white to light brown solid powder
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| 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)
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| Solubility (In Vitro) |
DMSO : 125 mg/mL (223.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (8.95 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 50.0 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. Solubility in Formulation 2: ≥ 5 mg/mL (8.95 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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