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Purity: ≥98%
NG 52 (NG-52), a tri-substituted purine, is a cell-permeable, reversible, and ATP-competitve inhibitor of the cell cycle-regulating kinase, Cdc28p with IC50 of 7 μM, and the related Pho85p kinase with IC50 of 2 μM. NG-52 inhibits Cdc28p and Pho85p by attaching to the ATP-binding site of yeast cyclin-dependent kinases.
| Targets |
cdc2-cyclin B (IC50 = 0.34 μM); Pho85p (IC50 = 2 nM); Cdc28p (IC50 = 7 μM); Phosphoglycerate kinase 1 (PGK1) (IC50 = 2.5 μM)
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| ln Vitro |
NG 52 (Compound 52) stops drug-sensitized S cells from growing. strains of cerevisiae that have a 30 μM GI50. With an IC50 value of 340 nM, NG 52 has activity against cdc2-cyclin B[1]. While primary astrocyte proliferation is efficiently inhibited, NG 52 dose-regulatedly decreases the GI50 values of neuroastrocytoma U87 and U251 cell lines to 7.8 μM and 5.2 μM, respectively [2]. In U87 and U251 cells, NG 52 (12.5-50 μM) efficiently suppresses the phosphorylation of PDH at Ser293 and PDHK1 at Thr338. This increases the amount of pyruvate that enters the Krebs cycle, which in turn increases ATP and ROS. manufacturing[2]. By suppressing the activity of PGK1, NG 52 increases the activity of pyruvate dehydrogenase (PDH), which reverses the Warburg effect and shifts oxygen-assisted cells from anaerobic to aerobic mode [2].
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| ln Vivo |
Neuronal tumor xenograft growth is inhibited by dose-regulated NG 52 (50-150 mg/kg; basal; daily; for 13 days) [2].
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: Glioma U87 and U251 Cell Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: 6 days Experimental Results: Effectively inhibited the proliferation of primary glioma cells. Western Blot Analysis [2] Cell Types: glioma U87 and U251 cells Tested Concentrations: 0 μM, 12.5 μM, 25 μM, 50 μM Incubation Duration: 12 hrs (hours) or 24 hrs (hours) Experimental Results: Effectively inhibited the proliferation of primary glioma cells. |
| Animal Protocol |
Animal/Disease Models: Female nu/nu (nude) mice (5-week old) injected with glioma cells [2]
Doses: 50 mg/kg, 100 mg/kg, 150 mg/kg Route of Administration: oral; daily; continued for 13 Day Experimental Results: Dose-dependent inhibition of glioma xenograft growth. |
| References |
[1]. ray NS, Wodicka L, Thunnissen AM et al. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998 Jul 24;281(5376):533-8.
[2]. Wen-Liang Wang, et al. Pharmacologically inhibiting phosphoglycerate kinase 1 for glioma with NG52. Acta Pharmacol Sin. 2020 Jul 31. |
| Molecular Formula |
C16H19CLN6O
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|---|---|
| Molecular Weight |
346.81466
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| Exact Mass |
346.13
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| Elemental Analysis |
C, 55.41; H, 5.52; Cl, 10.22; N, 24.23; O, 4.61
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| CAS # |
212779-48-1
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| Related CAS # |
212779-48-1
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| Appearance |
Solid powder
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| SMILES |
CC(C)N1C=NC2=C(N=C(N=C21)NCCO)NC3=CC(=CC=C3)Cl
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| InChi Key |
XZEFMZCNXDQXOZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19ClN6O/c1-10(2)23-9-19-13-14(20-12-5-3-4-11(17)8-12)21-16(18-6-7-24)22-15(13)23/h3-5,8-10,24H,6-7H2,1-2H3,(H2,18,20,21,22)
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| Chemical Name |
2-[[6-(3-chloroanilino)-9-propan-2-ylpurin-2-yl]amino]ethanol
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| Synonyms |
NG 52; NG52; NG-52; Compound 52
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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: 69~75 mg/mL (199~216.3 mM)
Ethanol: ~23 mg/mL (~66.3 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.21 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 (7.21 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8834 mL | 14.4171 mL | 28.8342 mL | |
| 5 mM | 0.5767 mL | 2.8834 mL | 5.7668 mL | |
| 10 mM | 0.2883 mL | 1.4417 mL | 2.8834 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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