2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid
- Product Name
- 2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid
- CAS No.
- 881487-77-0
- Chemical Name
- 2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid
- Synonyms
- KPT-6566;KPT-6566 (KPT 6566;KPT-6566, 10 mM in DMSO;KPT 6566;KPT6566;881487-77-0;2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid;Acetic acid, 2-[[4-[[[4-(1,1-dimethylethyl)phenyl]sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]thio]-;inhibit,Cyclin D1,ROS,KPT6566,breast epithelial,anti- proliferation,KPT 6566,Inhibitor,KPT-6566,DNA damage
- CBNumber
- CB64797854
- Molecular Formula
- C22H21NO5S2
- Formula Weight
- 443.54
- MOL File
- 881487-77-0.mol
2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid Property
- Boiling point:
- 622.4±65.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light, stored under nitrogen
- solubility
- DMSO: soluble
- form
- A solid
- pka
- 3.52±0.10(Predicted)
- color
- White to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML4010
- Product name
- KPT-6566
- Purity
- ≥98% (HPLC)
- Packaging
- 1 unit
- Price
- $405
- Updated
- 2025/07/31
- Product number
- DC11276
- Product name
- KPT-6566
- Purity
- >98%
- Packaging
- 1g
- Price
- $3800
- Updated
- 2021/12/16
2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid Chemical Properties,Usage,Production
Uses
KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer[1].
Biological Activity
Potent and selective peptidyl-prolyl cis-trans isomerase (PPIase) Pin1 covalent inhibitor with anti-cancer efficacy in cultures and in vivo.
KPT-6566 is a potent and selective peptidyl-prolyl cis-trans isomerase (PPIase) Pin1 inhibitor (IC50 = 640 nM) th at targets Pin1 catalytic site for covalent modification, resulting in Pin1 degradation and the release of ROS-generating and DNA-damaging quinone-mimicking KPT-6566-B. KPT-6566 inhibits the proliferation of wild-type, but not Pin1-/-, MEFs (1-5 μM for 48h) with concomitant reduction of cellular pRB and Cyclin D1 hyperphosphorylation. KPT-6566 induces cancer cell death in cultures (1-10 μM for 48h) and reduces MDA-MB-231 lung metastasis in mice in vivo (5 mg/kg/d i.p.). KPT-6566 is more potent than juglone and does not affect the PPIase activity of GST-FKBP4 or GST-PPIA.
in vivo
KPT-6566 (5 mg/kg; i.p. once a day for 26 days) shows no toxicity to mice[1].
| Animal Model: | 6-week-old female mice with 1 million of MDA-MB-231Luc6 cells injection[1] |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; 5 mg/kg once a day; for 26 days |
| Result: | Exibited no sign of local or systemic and organ toxicity by post mortem morphologic analyses. |
References
[1] Campaner E, et al. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nat Commun. 2017 Jun 9;8:15772. DOI:10.1038/ncomms15772
2-[[4-[[[4-(tert-Butyl)phenyl]sulfonyl]imino]-1-oxo-1,4-dihydro-2-naphthyl]thio]acetic Acid Preparation Products And Raw materials
Raw materials
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