Description du produit
.cp_wz table {border-top : 1px solide #ccc;border-left:1px solide #ccc ; } .cp_wz table td{border-right : 1px solide #ccc ; border-bottom : 1px solide #ccc ; remplissage : 5px 0px 0px 5px;} .cp_wz table th {border-right : 1px solid #ccc;border-bottom : 1px solid #ccc ; rembourrage : 5px 0px 0px 5px;}
Poids moléculaire :
322.42 INH6 est un puissant inhibiteur de Hec1, qui perturbe spécifiquement l'interaction Hec1/Nek2 et provoque un mauvais alignement des chromosomes.
Activité biologique
|
Description
|
INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
|
|
Targets
|
Hec1 [1]
|
|
In vitro
|
INH6 effectively targets the Hec1/Nek2 complex for degradation, and shows potent cell killing activity with IC50 of 1.7, 2.1, 2.4, and 2.5 μM in MDA-MB231, MDA-MB468, HeLa and K562 cell lines. INH6 also triggers mitotic abnormalities in HeLa cells, and induces apoptosis.
|
|
In vivo
|
|
|
Features
|
|
Protocole (uniquement pour référence) Dosage cellulaire : [1]
|
Cell lines
|
MDA-MB231, MDA-MB468, HeLa and K562 cell lines
|
|
Concentrations
|
~40 μM
|
|
Incubation Time
|
4 days
|
|
Method
|
Standard XTT assays with a four-day drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH analogs in cultured cells. Triplicate sets are measured and compiled for final data presentation. The assay is performed by using a commercial kit following the instructions. In principle, cells are plated on 96-well dishes one day before the drug treatment, followed by drug treatment on day 2 and XTT assay on day 5 after drug addition. The absorption at 595 nm is measured with a plate reader and converted to cell survival percentages in comparison to mock treated groups.
|
Conversion de différents animaux modèles sur la base de la BSA (valeur basée sur les données des lignes directrices provisoires de la FDA)
|
Species
|
Baboon
|
Dog
|
Monkey
|
Rabbit
|
Guinea pig
|
Rat
|
Hamster
|
Mouse
|
|
Weight (kg)
|
12
|
10
|
3
|
1.8
|
0.4
|
0.15
|
0.08
|
0.02
|
|
Body Surface Area (m2)
|
0.6
|
0.5
|
0.24
|
0.15
|
0.05
|
0.025
|
0.02
|
0.007
|
|
Km factor
|
20
|
20
|
12
|
12
|
8
|
6
|
5
|
3
|
|
Animal A (mg/kg) = Animal B (mg/kg) multiplied by
|
Animal B Km
|
|
Animal A Km
|
Par exemple, pour modifier la dose de resvératrol utilisée pour une souris (22,4 mg/kg) à une dose basée sur la BSA pour un rat, multiplier 22,4 mg/kg par le facteur Km pour une souris puis diviser par le facteur Km pour un rat. Ce calcul donne une dose équivalente chez le rat pour le resvératrol de 11,2 mg/kg.
|
Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
|
mouse Km(3)
|
= 11.2 mg/kg
|
|
rat Km(6)
|
Informations chimiques
|
Molecular Weight (MW)
|
322.42
|
|
Formula
|
C19H18N2OS
|
|
CAS No.
|
1001753-24-7
|
|
Storage
|
3 years -20℃Powder
|
|
6 months-80℃in solvent (DMSO, water, etc.)
|
|
Synonyms
|
N/A
|
|
Solubility (25°C) *
|
In vitro
|
DMSO
|
64 mg/mL
heating
(198.49 mM)
|
|
Water
|
<1 mg/mL
(
|
|
Ethanol
|
11 mg/mL
heating
(34.11 mM)
|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|
|
Chemical Name
|
N-[4-(2,4,6-trimethylphenyl)-2-thiazolyl]-benzamide
|
Calculateur de molarité Calculateur de dilution Calculateur de poids moléculaire
Groupes de Produits : Signalisation cytosquelettique > Inhibiteur associé aux microtubules
