N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide Chemical Properties

Melting point:

216-217 °C(Solv: ethanol (64-17-5))

Density 

1.27±0.1 g/cm3(Predicted)

storage temp. 

Keep in dark place,Sealed in dry,Room Temperature

solubility 

DMSO: ≥20mg/mL

form 

powder

pka

8.61±0.40(Predicted)

color 

white to off-white

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month.

Safety Information

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

1

N-(4-Acetyl-4,5-dihydro-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide Usage And Synthesis

Description

K858 (72926-24-0) is a selective mitotic kinesin Eg5 inhibitor (IC50 = 1.3 μM) which acts in an ATP-noncompetitive manner.1,2?It is at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. K-858 blocks centrosome separation, activates the spindle checkpoint and induces mitotic arrest accompanied by the formation of monopolar spindles. Displays no effect on microtubule polymerization. Selectively displays antiproliferative effects via induction of mitotic cell death in cancer cells over nontransformed cells.1

Uses

K 858 is a selective ATP-uncompetitive mitotic kinesin Eg5 inhibitor.

Definition

ChEBI: N-(4-acetyl-5-methyl-5-phenyl-1,3,4-thiadiazol-2-yl)acetamide is a member of benzenes.

References

1) Nakai et al. (2009), K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells; Cancer Res., 69 3901 2) Indorato et al. (2013), STLC-resistant cell lines as tools to classify chemically divergent Eg5 targeting agents according to their mode of action and target specificity; Biochem. Pharmacol.,?86?1441

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