| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
GJ103 (10-30 μM; 4 days) sodium promotes ATM folding activity in AT153LA cells with homozygous TGA mutations and homozygous TAA mutations [1]. GJ103 salt showed no appreciable active cytotoxicity on AT cells at doses as high as 300 µM [1].
|
|---|---|
| ln Vitro |
GJ103 (10-30 μM; 4 days) sodium promotes ATM folding activity in AT153LA cells with homozygous TGA mutations and homozygous TAA mutations [1]. GJ103 salt showed no appreciable active cytotoxicity on AT cells at doses as high as 300 µM [1].
GJ103 (an analog of GJ072) demonstrated read-through activity in A-T lymphoblastoid cell lines carrying homozygous nonsense mutations in the ATM gene. It induced ATM kinase activity, shown by increased ATMpSer1981 autophosphorylation and SMC1pSer966 transphosphorylation measured by flow cytometry (∆FI), and promoted ATMpSer1981 foci formation after irradiation (IRIF). The activity was observed in cells with TGA, TAG, and TAA stop codons at concentrations of 10 and 30 µmol/L. [1] GJ103 also induced detectable full-length ATM protein in A-T cells as measured by ATM-ELISA. [1] GJ103 and other GJ072 analogs did not show obvious cytotoxicity in A-T cells at concentrations up to 300 µmol/L. [1] |
| Cell Assay |
ATM kinase activity was assessed using flow cytometry for ATMpSer1981 and SMC1pSer966 phosphorylation. Cells were treated with compounds for 4 days, irradiated with 10 Gy, fixed, permeabilized, and stained with primary antibodies followed by fluorescent secondary antibodies. Fluorescence intensity was measured by flow cytometry. [1]
ATMpSer1981 nuclear foci formation (IRIF) was evaluated by immunofluorescence. After 4-day compound treatment, cells were irradiated with 2 Gy, fixed, permeabilized, blocked, and incubated with anti-ATMpSer1981 antibody followed by FITC-conjugated secondary antibody. Foci were visualized and quantified microscopically. [1] Full-length ATM protein levels were measured by ATM-ELISA using nuclear extracts from compound-treated cells. [1] Cytotoxicity was assessed by XTT assay after compound treatment, measuring absorbance at 480 nm. [1] |
| References | |
| Additional Infomation |
GJ103 is a water-soluble salt form of the GJ072 analogue, designed for convenient in vivo administration. [1]
It belongs to a family of small molecule read-through (SMRT) compounds that induce early read-through of stop codons, thus providing a potential therapeutic strategy for genetic diseases caused by nonsense mutations, such as capillary dilatational ataxia (AT). [1] This compound is effective against all three types of nonsense mutations (TGA, TAG, and TAA), which is considered beneficial for its translational application. [1] |
| Molecular Formula |
C16H15N4NAO3S
|
|---|---|
| Molecular Weight |
366.370072603226
|
| Exact Mass |
364.06
|
| Elemental Analysis |
C, 52.74; H, 3.60; N, 15.38; Na, 6.31; O, 13.17; S, 8.80
|
| CAS # |
1459687-96-7
|
| Related CAS # |
GJ103;1459687-89-8
|
| PubChem CID |
71748052
|
| Appearance |
Solid powder
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
25
|
| Complexity |
434
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
PTFQBXAUOWUATD-UHFFFAOYSA-M
|
| InChi Code |
InChI=1S/C16H14N4O3S.Na/c1-23-12-6-4-5-11(9-12)20-15(13-7-2-3-8-17-13)18-19-16(20)24-10-14(21)22;/h2-9H,10H2,1H3,(H,21,22);/q;+1/p-1
|
| Chemical Name |
sodium;2-[[4-(3-methoxyphenyl)-5-pyridin-2-yl-1,2,4-triazol-3-yl]sulfanyl]acetate
|
| Synonyms |
GJ-103 sodium;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~50 mg/mL (~137.23 mM)
H2O : ≥ 10 mg/mL (~27.45 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.86 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 25.0 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: ≥ 2.5 mg/mL (6.86 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 25.0 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: ≥ 2.5 mg/mL (6.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 2.7295 mL | 13.6474 mL | 27.2948 mL | |
| 5 mM | 0.5459 mL | 2.7295 mL | 5.4590 mL | |
| 10 mM | 0.2729 mL | 1.3647 mL | 2.7295 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
