| KX1-004Pp60c-src inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.83%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
KX1-004 Dilution Calculator
calculate
KX1-004 Molarity Calculator
calculate
| Cas No. | 518058-84-9 | SDF | Download SDF |
| Chemical Name | 5-fluoro-N-(3-hydroxybenzyl)-1H-indole-2-carboxamide | ||
| Canonical SMILES | FC1=CC(C=C(C(NCC2=CC=CC(O)=C2)=O)N3)=C3C=C1 | ||
| Formula | C16H13FN2O2 | M.Wt | 284.29 |
| Solubility | ≥10.1mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
KX1-004 is a non-ATP competitive inhibitor of pp60c-src with IC50 value of 40 μM [1].
KX1-004 is a close analog of the indole-based Src-PTK inhibitors reported previously. It has a 5-fluoro group and showed potent inhibition activity in isolated Src-PTK assay. KX1-004 was found to have protective effect in noise-induced hearing loss. The chinchillas treated with 30 μM KX1-004 were exposed to continuous noise. And the results showed that treated ears exhibited up to 40 dB less threshold shift (TTS) and up to 25 dB less permanent threshold shift (PTS) than control ears. KX1-004 treatment also significantly reduced outer hair cell (OHC) loss than control. Besides that, KX1-004 was proved to reduce the hearing loss and hair cell loss associated with impulse noise exposure markedly [1, 2].
References:[1] Harris K C, Hu B, Hangauer D, et al. Prevention of noise-induced hearing loss with Src-PTK inhibitors. Hearing research, 2005, 208(1): 14-25.[2] Milkiewicz K L, Marsilje T H, Woodworth Jr R P, et al. The design, synthesis and activity of non-ATP competitive inhibitors of pp60 c-src tyrosine kinase. Part 2: Hydroxyindole derivatives. Bioorganic & medicinal chemistry letters, 2000, 10(5): 483-486.
