PhiKan-083 Hydrochloride
- CAS No.
- 880813-36-5
- Chemical Name:
- PhiKan-083 Hydrochloride
- Synonyms
- PK083;PhiKan 083;PhiKan-083 Hydrochloride;9-Ethyl-N-methyl-carbazole-3-methanamine;9H-Carbazole-3-methanamine, 9-ethyl-N-methyl-;[(9-Ethyl-9H-carbazol-3-yl)methyl](methyl)amine;9-Ethyl-N-methyl-9H-carbazole-3-methanamine hydrochloride;PhiKan 083,PhiKan-083,Inhibitor,MDM-2/p53,PhiKan083,inhibit
- CBNumber:
- CB02652533
- Molecular Formula:
- C16H18N2
- Molecular Weight:
- 238.33
- MDL Number:
- MFCD07366384
- MOL File:
- 880813-36-5.mol
- MSDS File:
- SDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P264-P270-P301+P312-P330-P501-P264-P280-P302+P352-P321-P332+P313-P362-P264-P280-P305+P351+P338-P337+P313P |
PhiKan-083 Hydrochloride price More Price(19)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Tocris | 4326 | PhiKan083 ≥99%(HPLC) | 880813-36-5 | 10 | $199 | 2021-12-16 | Buy |
| Tocris | 4326 | PhiKan083 ≥99%(HPLC) | 880813-36-5 | 50 | $788 | 2021-12-16 | Buy |
| Usbiological | 256233 | PhiKan 083 | 880813-36-5 | 10mg | $446 | 2021-12-16 | Buy |
| AK Scientific | 1949CN | 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine | 880813-36-5 | 100mg | $714 | 2021-12-16 | Buy |
| AK Scientific | 1949CN | 1-(9-Ethyl-9H-carbazol-3-yl)-N-methylmethanamine | 880813-36-5 | 250mg | $727 | 2021-12-16 | Buy |
PhiKan-083 Hydrochloride Chemical Properties,Uses,Production
Uses
PhiKan-083 is a p53 stabilizing agent. PhiKan-083 preferentially binds mutated (Y220C) p53 over wild-type p53 at a site distinct from functional DNA/protein interaction regions. PhiKan-083 slows rate of thermal denaturation of p53-Y220C.
Biological Activity
ki: ≈ 150 mphikan 083 is a critical p53 stabilizing agent by bonding its mutation y220cthe mutation y220c of p53 exists a surface cavity that destabilizes the protein by 4 kcal/mol, at a site that is not functional. a p53 stabilizing agent binding it is able to slow rate of thermal denaturation [1].
in vitro
isothermal titration of phikan083 with t-p53c-y220c exhibited 1:1 stoichiometry and a kd of 125 ± 10 m. phikan083 stabilized t-p53c-y220c in a concentration-dependent manner. in a simple binding model for phikan083 (t-p53c-y220c at 310 k (37°c)), in the absence of ligand, the protein gave a half-life of 3.8 min, while it increased to 15.7 min at saturating concentrations of phikan083. this is a proposed anticancer drug that could be developed for the y220c mutant using p53 stabilizing agent. the site of mutation in the oncogenic y220c mutant phikan083 binds with reasonable affinity is a druggable target. interestingly, the site of mutation does not exist in a region of the protein that is functionally important, it will be an excellent target for drug stabilization therapy. this suggests the crystal structure of the complex will be a fresh start for further rounds of drug design and refinement [1].
References
[1] boeckler fm, joerger ac, jaggi g, rutherford tj, veprintsev db, fersht ar. 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.
PhiKan-083 Hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
PhiKan-083 Hydrochloride Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Nextpeptide Inc | +86-0571-81612335 +8613336028439 | sales@nextpeptide.com | China | 19915 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42057 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| J & K SCIENTIFIC LTD. | 010-82848833 400-666-7788 | jkinfo@jkchemical.com | China | 96815 | 76 |
| EMMX Biotechnology LLC | 888-539-0666 | info@emmx.com | United States | 8449 | 60 |
| Changzhou Hopschain Chemical Co.,Ltd. | 0519-85528066 13775048983 | sales@hopschem.com | China | 31557 | 55 |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2985 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 18892239720 | psaitong@jm-bio.com | China | 12308 | 58 |
| MQ (shanghai) Pharmaceuticals Co., Ltd. | 13761635123 | 1014988033@qq.com | China | 4979 | 55 |