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Purity: ≥98%
1,4-DPCA is a novel, potent and competitive inhibitor of prolyl 4-hydroxylase with IC50 value of 3.6 μM. Increased collagen deposition provides physical and biochemical signals to support tumor growth and invasion during breast cancer development. Therefore, inhibition of collagen synthesis and deposition has been considered a strategy to suppress breast cancer progression. Collagen prolyl-4-hydroxylase α subunit 2 (P4HA2), an enzyme hydroxylating proline residues in -X-Pro-Gly- sequences, is a potential therapeutic target for the disorders associated with increased collagen deposition. However, expression and function of P4HA2 in breast cancer progression are not well investigated.
| ln Vitro |
In mouse B6 cells, 1,4-DPCA (24 hours) can treat many elevated target gene expressions, such as the pro-angiogenic target genes Vegfa and Hmox1 and the pro-glycolytic target genes Ldh-a, Pgk1, Pdk1, and 1. ZR-75-1 (20 μM 1,4-DPCA) and T4-2 (10 μM 1,4-DPCA) cells showed a significant reduction in colony size following 4-DPCA therapy. In three-dimensional culture, T4-2 cells treated with DPCA produced localized spheroids. Treatment with 1,4-DPCA significantly decreased MDA-MB-231 (10 μM 1,4-DPCA), ZR-75-1, MDA-MB-157, and T4-2 cells [3].
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| ln Vivo |
In intravascular peritoneal poly(lock-co-glycolic acid) (PLGA) discs, treatment with 1,4-DPCA successfully prevented connective tissue ingrowth for a period of 28 days. The pivot disc's intra- and exterior surface-restricted collagen deposition as well as connective tissue ingrowth are successfully inhibited by 1,4-DPCA capture, though not to the same degree as glucocorticoids [2].
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| References |
| Molecular Formula |
C13H8N2O3
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|---|---|---|
| Molecular Weight |
240.22
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| Exact Mass |
240.053
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| CAS # |
331830-20-7
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| Related CAS # |
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| PubChem CID |
459803
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
474.5±45.0 °C at 760 mmHg
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| Flash Point |
240.8±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.727
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| LogP |
3.28
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
419
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XZZHOJONZJQARN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8N2O3/c16-12-8-4-3-7-2-1-5-14-10(7)11(8)15-6-9(12)13(17)18/h1-6H,(H,15,16)(H,17,18)
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.92 mg/mL (3.83 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 9.2 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: 10 mg/mL (41.63 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 4.1629 mL | 20.8143 mL | 41.6285 mL | |
| 5 mM | 0.8326 mL | 4.1629 mL | 8.3257 mL | |
| 10 mM | 0.4163 mL | 2.0814 mL | 4.1629 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.
Treatment with P4HA inhibitor attenuates breast cancer cell proliferation and invasiveness.BMC Cancer. 2014; 14: 1. |
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Reducing P4HA2 expression or inhibiting its activity impairs collagen deposition.BMC Cancer. 2014; 14: 1. |
Knockdown of P4HA2 suppresses tumor growth and metastasisin vivo.BMC Cancer. 2014; 14: 1. |
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