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533916 Sigma-AldrichKIFC1 Inhibitor, AZ82 - CAS 1449578-65-7 - Calbiochem

A cell-permeable, potent and selective inhibitor of MT-bound KIFC1 motor domain ATPase activity. Targets centrosome-amplified tumor cells, causes mitotic delay & multipolar spindle formation.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: 5-Methyl-N-((R)-1-oxo-1-((R)-pyrrolidin-3-ylamino)-3-(6-(3-(trifluoromethoxy)phenyl)pyridin-3-yl)propan-2-yl)-4-propylthiophene-2-carboxamide, Tctex7 Inhibitor, Knsl2 Inhibitor, MT/KIFC1 Inhibitor, Bm4137 Inhibitor, HSET Inhibitor, Kinesin Family Member C1 Inhibitor

Primary Target: MT/KIFC1

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1449578-65-7	C₂₈H₃₁F₃N₄O₃S

价格及供货情况

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Description
Overview	A cell-permeable pyridinylpropanylthiophene-carboxamide compound that acts as a potent, reversible, and ATP-competitive (K_i = 43 nM) and microtubule (MT) non-competitive inhibitor of MT-stimulated ATPase activity of KIFC1 (IC₅₀ = 300 nM). However, it does not affect the basal ATPase activity even at high concentrations (~100 µM). Binds to the MT/KIFC1 complex (K_d of 690 nM) with high-affinity and blocks ATP binding and release of ADP. Does not directly interact with KIFC protein that is not associated with MT. Exhibits high degree of selectivity against a panel of nine kinesin motor proteins at a concentration (~ 5 µM) where KIFC1 activity is reduced by 95%. Causes mitotic delay, multipolar spindle formation and centrosome declustering in centrosome-amplified BT-549 cancer cells without affecting normal cells. Also shown to prevent Eg5 inhibition induced monopolar spindles and restores bipolar mitotic spindle formation in HeLa cells at 400 nM.
Catalogue Number	533916
Brand Family	Calbiochem®
Synonyms	5-Methyl-N-((R)-1-oxo-1-((R)-pyrrolidin-3-ylamino)-3-(6-(3-(trifluoromethoxy)phenyl)pyridin-3-yl)propan-2-yl)-4-propylthiophene-2-carboxamide, Tctex7 Inhibitor, Knsl2 Inhibitor, MT/KIFC1 Inhibitor, Bm4137 Inhibitor, HSET Inhibitor, Kinesin Family Member C1 Inhibitor
Description	KIFC1 Inhibitor, AZ82

References
References	Reference: Wu, J., et al. 2013. ACS Chem. Biol. 8, 2201.

Product Information
CAS number	1449578-65-7
Form	Yellow film
Hill Formula	C₂₈H₃₁F₃N₄O₃S
Chemical formula	C₂₈H₃₁F₃N₄O₃S
Reversible	Y
Quality Level	MQ100

Applications

Biological Information
Primary Target	MT/KIFC1
Purity	≥96% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.33916.0001	04055977281569

Documentation

KIFC1 Inhibitor, AZ82 - CAS 1449578-65-7 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Reference: Wu, J., et al. 2013. ACS Chem. Biol. 8, 2201.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	07-August-2017 JSW
Synonyms	5-Methyl-N-((R)-1-oxo-1-((R)-pyrrolidin-3-ylamino)-3-(6-(3-(trifluoromethoxy)phenyl)pyridin-3-yl)propan-2-yl)-4-propylthiophene-2-carboxamide, Tctex7 Inhibitor, Knsl2 Inhibitor, MT/KIFC1 Inhibitor, Bm4137 Inhibitor, HSET Inhibitor, Kinesin Family Member C1 Inhibitor
Description	A cell-permeable pyridinylpropanylthiophene-carboxamide compound that exhibits selective affinity toward MT/microtubule-bound KIFC1 motor domain (Q305-K673; K_d = 690 nM), but not to uncomplexed KIFC1 or MT, and selectively inhibits MT-induced, but not basal, KIFC1 motor domain ATPase activity (IC₅₀ = 300 nM; [KIFC1] = 30 nM, [MT] = 100 nM, [ATP] = 15 µM) in an ATP-competitive (K_i = 43 nM; [KIFC1] = 125 nM, [MT] = 1.5 µM) and MT-noncompetitive manner, effectively preventing ADP release, while displaying little potency against 9 other kinesin motor proteins (<15% or no inhibition at 5 µM against human CENP-E, Chromokinesin/KIF4A, Eg5, KIFC3, KIF3C, KInesin Heavy Chain/KIF5B, MCAK/KIF2C, MKLP1/KIF23, and A. nidulans BimC/KIF8). KIFC1 knockdown by siRNA or functional inhibition by AZ82 (0.4 to 1.2 µM) is shown to result in mitotic delay and multipolar spindle formation among BT549 population with extra centrosomes due to failure of chromosomes clustering. In cells with normal/two centrosomes, Eg5 inhibition causes monopolar spindles formation, while AZ82 co-treatment (400 nM) offsets the effect of Eg5 inhibition (5 nM AZD4877) and restores bipolar spindles phenotype in mitotic HeLa cells. Off-target cytotoxicity is reported when used at concentrations above 4 µM.
Form	Yellow film
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1449578-65-7
Chemical formula	C₂₈H₃₁F₃N₄O₃S
Purity	≥96% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Reference: Wu, J., et al. 2013. ACS Chem. Biol. 8, 2201.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > ATPase/GTPase Inhibitors > ATPase Inhibitors

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