| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
PGMI-004A inhibits PGAM1 with an IC50 of about 13.1 μM, and the PGMI-004A-PGAM1 response's fluorescence-determined Kd value is 7.2 μM. To control PGAM1 activity, PGMI-004A can alter the structure of the enzyme. The protein-ligand complex's Kd value was computed to be 9.4 μM, and the Ki value was found to be 3.91 μM using Dixon plot analysis. PGMI-004A (20 μM) treatment inhibiting PGAM1 activity led to lower 2-PG and higher 3-PG levels in H1299 cells, which could be restored by methyl-2-PG treatment. Lactate production was significantly reduced after treatment with PGMI-004A (20 μM), and intracellular ATP levels were not significantly affected by treatment with methyl 2-PG, but lactate production was restored. Treatment with PGMI-004A (20 μM) decreased the amount of oxidized PPP and NADPH/NADP+ amplification, caused anemia, decreased RNA biosynthesis, and decreased H1299 cell proliferation. Human cancer and leukemia cells treated with PGMI-004A showed decreased cell proliferation, while human dermal fibroblasts (HDF), human foreskin fibroblasts (HFF), human cells pretreated with HaCaT, and human melanopiginated PIG1 cells did not show this effect. PGMI-004A's minimally non-toxic effects on normally proliferating human cells are indicated [1].
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| ln Vivo |
In xenograft research, mice that were not clothed were given injections of H1299 cells. Volunteers (n = 8/group) received PGMI-004A (100 mg/kg/day) or vehicle for 21 days following injection, starting six days after the injection. When PGMI-004A was administered to treated mice, compared to vehicle-control mice, there were notable decreases in tumor growth and size. Furthermore, xenografted nude mouse tumors' PGAM1 enzyme activity can be successfully inhibited by PGMI-004A therapy [1].
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| References |
| Molecular Formula |
C21H12F3NO6S
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|---|---|
| Molecular Weight |
463.3832
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| Exact Mass |
463.034
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| CAS # |
1313738-90-7
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| PubChem CID |
66521681
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.846
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
849
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XKVNBCMGEUDKNP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H12F3NO6S/c22-21(23,24)10-5-7-11(8-6-10)25-32(30,31)15-9-14-16(20(29)19(15)28)18(27)13-4-2-1-3-12(13)17(14)26/h1-9,25,28-29H
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| Chemical Name |
3,4-dihydroxy-9,10-dioxo-N-[4-(trifluoromethyl)phenyl]anthracene-2-sulfonamide
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| Synonyms |
PGMI 004A; PGMI004A; PGMI-004A
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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 : ≥ 50 mg/mL (~107.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.49 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 20.8 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: ≥ 2.08 mg/mL (4.49 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1581 mL | 10.7903 mL | 21.5806 mL | |
| 5 mM | 0.4316 mL | 2.1581 mL | 4.3161 mL | |
| 10 mM | 0.2158 mL | 1.0790 mL | 2.1581 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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