CAY10550

Names

[ Name ]:
CAY10550

[Synonym ]:
TCS PRP INHIBITOR 13
Necrosulfonamide
1-Phenyl-3-p-nitrophenylpyrazolon
3H-Pyrazol-3-one, 2,4-dihydro-5-(4-nitrophenyl)-2-phenyl-
5-(4-Nitrophenyl)-2-phenyl-2,4-dihydro-3H-pyrazol-3-one

Biological Activity

[Description]:

TCS PrP Inhibitor 13, an antiprion agent, is a cellular prion protein (PrPC) inhibitor. TCS PrP Inhibitor 13, as a protease-resistant form of prion protein (PrP-res) accumulation inhibitor, shows an IC50 value of 3 nM in both ScN2a and F3 cell lines. TCS PrP Inhibitor 13 induces Schwannoma cells apoptosis[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Research Areas >> Infection

[Target]

IC50: 3 nM (PrPC in ScN2a and F3 cells)[1]

[In Vitro]

TCS PrP Inhibitor 13 (0~500 μM; Schwannoma cells) significantly reduces levels of total ERK1/2, pAKT, total FAK, Cyclin D1, PrPC and significantly increases expression of cleaved caspase-3. TCS PrP Inhibitor 13 (Schwannoma cells) significantly reduces the number of proliferating, Ki67-positive cells and total cell number[2].

[References]

[1]. Kimata A, et al. New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation [published correction appears in J Med Chem. 2008 Mar 13;51(5):1503]. J Med Chem. 2007;50(21):5053-5056.

[2]. Provenzano L, et al. Cellular prion protein (PrPC) in the development of Merlin-deficient tumours. Oncogene. 2017;36(44):6132-6142.

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
445.1±47.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₅H₁₁N₃O₃

[ Molecular Weight ]:
281.27

[ Flash Point ]:
223.0±29.3 °C

[ Exact Mass ]:
281.080048

[ PSA ]:
78.49000

[ LogP ]:
1.92

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.674

Safety Information

[ HS Code ]:
2933199090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933199090

[ Summary ]:
2933199090. other compounds containing an unfused pyrazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%