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Merck

324622

Eg5 Inhibitor III, Dimethylenastron

The Eg5 Inhibitor III, Dimethylenastron, also referenced under CAS 863774-58-7, controls the biological activity of Eg5. This small molecule/inhibitor is primarily used for Membrane applications.

동의어(들):

Eg5 Inhibitor III, Dimethylenastron, 7,7-Dimethyl-4-(3-hydroxyphenyl)-5-oxo-3,4,5,6,7,8-hexahydroquinazolin-2(1H)-thione

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크기 선택


제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C16H18N2O2S
CAS 번호:
Molecular Weight:
302.39
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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SMILES string

S=C1NC(C3=C(N1)CC(CC3=O)(C)C)c2cc(ccc2)O

InChI

1S/C16H18N2O2S/c1-16(2)7-11-13(12(20)8-16)14(18-15(21)17-11)9-4-3-5-10(19)6-9/h3-6,14,19H,7-8H2,1-2H3,(H2,17,18,21)

InChI key

RUOOPLOUUAYNPY-UHFFFAOYSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

white to light yellow

solubility

DMSO: 10 mg/mL, methanol: 5 mg/mL

shipped in

ambient

Quality Level

storage temp.

2-8°C

General description

A cell-permeable quinazoline-thione compound that acts as a potent, specific, and reversible inhibitor of the microtubule-stimulated ATPase activity of the mitotic motor, Eg5 (IC50 = 200 nM). Exhibits little effect on the ATPase activity of kinesin-1, -4, -7 and -10 and is ~100-fold more potent than Monastrol (Cat. No. 475879). Also inhibits bipolar spindle formation in both HeLa cells and in Xenopus egg extracts and induces cell cycle arrest (~1 µM). Shown to induce mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Microtubule-stimulated ATPase activity of the mitotic motor
Product does not compete with ATP.
Reversible: yes
Target IC50: 200 nM inhibiting the microtubule-stimulated ATPase activity of the mitotic motor, Eg5

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Liu, M., et al. 2006. J. Biol Chem.in press.
Gartner, M., et al. 2005. Chembiochem6, 1173.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Harmful (C)

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


시험 성적서(COA)

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문서 라이브러리 방문

Mostafa A Aboouf et al.
Scientific reports, 13(1), 14514-14514 (2023-09-05)
Extravehicular activities, the backbone of manned space exploration programs, set astronauts into mild hypoxia. Unfortunately, microgravity aggravates threatening symptoms of hypoxia such as vision impairment and brain edema. Hypoxia-inducible factors (HIFs) sense cellular hypoxia and, subsequently, change the cells' expression
Stephen DiGiuseppe et al.
Proceedings of the National Academy of Sciences of the United States of America, 113(22), 6289-6294 (2016-05-18)
During the entry process, the human papillomavirus (HPV) capsid is trafficked to the trans-Golgi network (TGN), whereupon it enters the nucleus during mitosis. We previously demonstrated that the minor capsid protein L2 assumes a transmembranous conformation in the TGN. Here
Roshan L Shrestha et al.
The Journal of cell biology, 220(4) (2021-02-24)
Chromosomal instability (CIN) is a hallmark of many cancers. Restricting the localization of centromeric histone H3 variant CENP-A to centromeres prevents CIN. CENP-A overexpression (OE) and mislocalization have been observed in cancers and correlate with poor prognosis; however, the molecular

국제 무역 품목 번호

SKUGTIN
324622-5MGCN04055977197372

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