- ZCL278
| CasinGTPase Cdc42 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
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- Purity = 98.15%
- COA (Certificate Of Analysis)
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- NMR (Nuclear Magnetic Resonance)
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Chemical structure
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| Cas No. | 425399-05-9 | SDF | Download SDF |
| Chemical Name | 2-((6-phenyl-2,3,4,9-tetrahydro-1H-carbazol-1-yl)amino)ethanol | ||
| Canonical SMILES | OCCNC1CCCC2=C1NC3=C2C=C(C4=CC=CC=C4)C=C3 | ||
| Formula | C20H22N2O | M.Wt | 306.4 |
| Solubility | ≥30.6mg/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. | ||
IC50: 2 μM
CASIN is a selective GTPase Cdc42 inhibitor.
Cdc42 belongs to the family of small RhoGTPases and cycles between an active (GTP-bound) and an inactive (GDP-bound) state. In distinct cell types, Cdc42 has been known to regulate tubulin and actin organization, cell-cell and cell-extracellular matrix adhesion, as well as cell polarity.
In vitro: Previous study found that treatment with CASIN at 5μM reduced the elevated level of active Cdc42 observed in aged primitive hematopoietic cells to the level observed in young cells. However, CASIN treatment could not alter cell cycle status or apoptosis in aged LT-HSCs. Moreover, in response to the treatment of CASIN, LT-HSCs from aged mice had a dose-dependent increase in the percentage of polarized cells, which is progressively indistinguishable from young cells. In addition, though CASIN acted on Cdc42 activity transiently, the increase in the percentage of polar cells among aged LT-HSCs that were induced by CASIN could remain stable for at least up to 6 hr after the withdrawal of CASIN [1].
In vivo: Rat in-vivo study showed that CASIN could generated a rejuvenated phenotype of hematopoietic stem cells (HSCs), reversing the aging-related and polarity phenotype of aged HSCs to that of young HSCs [1].
Clinical trial: Up to now, CASIN is still in the preclinical development stage.
Reference:[1] Florian MC,Drr K,Niebel A,Daria D,Schrezenmeier H,Rojewski M,Filippi MD,Hasenberg A,Gunzer M,Scharffetter-Kochanek K,Zheng Y,Geiger H. Cdc42 activity regulates hematopoietic stem cell aging and rejuvenation. Cell Stem Cell.2012 May 4;10(5):520-30.
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