PhiKan 083 hydrochloride
Based on 1 publication(s) in Google Scholar
PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.
For research use only. We do not sell to patients.
- Purity: 99.27%
- CAS No.: 1050480-30-2
- Formula: C16H19ClN2
- Molecular Weight:274.79
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PhiKan 083 hydrochloride
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Biological Activity
Kd: 167 μM (p53-Y220C)[1], 150 μM (p53Y220C, in Ln229 cells)[3]
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM[1], shows a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3].
PhiKan 083 slows down its thermal denaturation rate[2].
PhiKan 083 (125 μM, 48 hours) reduces the cell viability of engineered variants of Ln229 cells[3].
PhiKan 083 (100 μM) in conbination with NSC 123127 (1 μM) enhances the pro-apoptotic activity in all variants of Ln229 cells (p53wt, p53Y220C, p53G245S, p53R282W)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W cells
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Concentration:125 μM
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Incubation Time:48 hours
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Result:Caused ∼70 ± 5% reduction in cell viability of variants of Ln229 cells.
Chemical Information
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CAS No. 1050480-30-2
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Appearance Solid
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Molecular Weight 274.79
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Formula C16H19ClN2
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Color White to off-white
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SMILES
CNCC1=CC2=C(C=C1)N(CC)C3=C2C=CC=C3.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
Impairing the interaction between Erg11 and cytochrome P450 reductase Ncp1 enhances azoles' antifungal activities. [Abstract]2025 Jul 24;16(1):6821. PMID: 40707518
Solvent & Solubility
DMSO : 62.5 mg/mL (227.45 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2 mg/mL (7.28 mM; Need ultrasonic and warming)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Boeckler FM, et al. Targeted rescue of a destabilized mutant of p53 by an in silico screened drug. Proc Natl Acad Sci U S A. 2008 Jul 29;105(30):10360-5. [Content Brief]
[2]. Rauf SM, et al. Effect of Y220C mutation on p53 and its rescue mechanism: a computer chemistry approach. Protein J. 2013 Jan;32(1):68-74. [Content Brief]
[3]. Paulmurugan R, et al. A protein folding molecular imaging biosensor monitors the effects of drugs that restore mutant p53 structure and its downstream function in glioblastoma cells. Oncotarget. 2018 Apr 20;9(30):21495-21511. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.6391 mL | 18.1957 mL | 36.3914 mL | 90.9786 mL |
| 5 mM | 0.7278 mL | 3.6391 mL | 7.2783 mL | 18.1957 mL | |
| DMSO | 10 mM | 0.3639 mL | 1.8196 mL | 3.6391 mL | 9.0979 mL |
| 15 mM | 0.2426 mL | 1.2130 mL | 2.4261 mL | 6.0652 mL | |
| 20 mM | 0.1820 mL | 0.9098 mL | 1.8196 mL | 4.5489 mL | |
| 25 mM | 0.1456 mL | 0.7278 mL | 1.4557 mL | 3.6391 mL | |
| 30 mM | 0.1213 mL | 0.6065 mL | 1.2130 mL | 3.0326 mL | |
| 40 mM | 0.0910 mL | 0.4549 mL | 0.9098 mL | 2.2745 mL | |
| 50 mM | 0.0728 mL | 0.3639 mL | 0.7278 mL | 1.8196 mL | |
| 60 mM | 0.0607 mL | 0.3033 mL | 0.6065 mL | 1.5163 mL | |
| 80 mM | 0.0455 mL | 0.2274 mL | 0.4549 mL | 1.1372 mL | |
| 100 mM | 0.0364 mL | 0.1820 mL | 0.3639 mL | 0.9098 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
PhiKan 083 hydrochloride Related Classifications
HY-108637A Related Classifications
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