5,15-DPP (Synonyms: 5,15-Diphenylporphyrin,STAT3 Inhibitor VIII) |
| Katalog-Nr.GC12138 |
5,15-DPP (5,15-DPP) ist ein selektiver STAT3-SH2-Antagonist (IC50s von 0,28 μM und 10 μM fÜr STAT3 bzw. STAT1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 22112-89-6
Sample solution is provided at 25 µL, 10mM.
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5,15-diphenylporphyrin (5,15-DPP) is a selective STAT3-SH2 antagonist [1].
Stat3 is constitutively activated in many human cancers. Stat3 functions as a critical mediator of oncogenic signaling through transcriptional activation of genes encoding apoptosis inhibitors, cell-cycle regulators and inducers of angiogenesis [2]. Aberrant STAT3 activity has been associated with transforming mechanisms induced by oncogenic tyrosine kinases [1].
In vitro: 5,15-DPP directly bound to STAT3 and antagonized the function of STAT3-SH2. 5,15-DPP selectively antagonized STAT3-SH2 with an IC50 of 0.28 μM over the other SH2-containing proteins STAT1 and Grb2[1]. The estimated KD values for the 5,15-DPP binding to STAT3 was 880 nM. Treatment with 5,15-DPP suppressed the DNA binding activity of STAT3 in a concentration-dependent manner. 5,15-DPP poorly inhibited STAT1 with an IC50 of 10 μM and showed no effect Grb2 [1].
References:
[1] Uehara Y, Mochizuki M, Matsuno K, et al. Novel high-throughput screening system for identifying STAT3–SH2 antagonists[J]. Biochemical and biophysical research communications, 2009, 380(3): 627-631.
[2] Jing N, Tweardy D J. Targeting Stat3 in cancer therapy[J]. Anti-cancer drugs, 2005, 16(6): 601-607.
| Cas No. | 22112-89-6 | SDF | |
| Überlieferungen | 5,15-Diphenylporphyrin,STAT3 Inhibitor VIII | ||
| Chemical Name | 5,15-diphenyl-21H,23H-porphine | ||
| Canonical SMILES | C1(C=C/2)=NC2=C/C3=CC=C(/C(C4=CC=CC=C4)=C5N=C(/C=C6N/C(C=C\6)=C1/C7=CC=CC=C7)C=C\5)N3 | ||
| Formula | C32H22N4 | M.Wt | 462.6 |
| Löslichkeit | ≤2mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1617 mL | 10.8085 mL | 21.6169 mL |
| 5 mM | 0.4323 mL | 2.1617 mL | 4.3234 mL |
| 10 mM | 0.2162 mL | 1.0808 mL | 2.1617 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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