Identification | Back Directory | [Name]
Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)- | [CAS]
2451481-08-4 | [Synonyms]
sulfopin Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)- | [Molecular Formula]
C11H20ClNO3S | [MDL Number]
MFCD32860123 | [MOL File]
2451481-08-4.mol | [Molecular Weight]
281.8 |
Chemical Properties | Back Directory | [Boiling point ]
455.5±45.0 °C(Predicted) | [density ]
1.23±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in DMSO (>25 mg/ml) | [form ]
solid | [pka]
-1.36±0.20(Predicted) | [color ]
Off-white | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
Hazard Information | Back Directory | [Description]
Sulfopin (2451481-08-4) is a potent and selective covalent inhibitor of peptidyl-prolyl isomerase NIMA interacting-1 (Pin1) (Ki = 17 nM).1 Although it displayed little to no cytotoxicity against a panel of 300 cancer cell lines, it had a significant impact on cancer cell growth after prolonged treatment. It suppressed MYCN-driven neuroblastoma initiation and the growth and survival of primary neuroblastoma tumor cell transplants in zebrafish. | [Uses]
Sulfopin (PIN1-3) is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17 nM. Sulfopin blocks Myc-driven tumors in vivo. The peptidyl-prolyl isomerase, Pin1, is exploited in cancer to activate oncogenes and inactivate tumor suppressors[1]. | [in vivo]
Sulfopin (40 mg/kg; p.o.; QD/BID for 7 days) regresses neuroblastoma in mice[1].
Sulfopin (20-40 mg/kg; i.p.; daily for 27 days) inhibits pancreatic cancer progression in mice[1].
Sulfopin (25-100 μM) blocks neuroblastoma in zebrafish[1]. Animal Model: | Transgenic Th-MYCN mice[1] | Dosage: | 40 mg/kg | Administration: | Once a day (QD) or twice a day (BID) for 7 days | Result: | Sulfopin-treated QD mice showed a significant average increase in survival of 10 days, while Sulfopin-treated BID mice showed an even more pronounced average increase of 28 days.
|
| [References]
Dubiella et al. (2021), Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo; Nat. Cham. Biol. 17 954 |
|
Company Name: |
DC Chemicals
|
Tel: |
021-58447131 13564518121 |
Website: |
www.chemicalbook.com/showsupplierproductslist927327/0.htm |
|