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506305 Sigma-AldrichSKP2 E3 Ligase Inhibitor III - Calbiochem

SKP2 E3 Ligase Inhibitor III - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCF^SKP2 Inhibitor III, SZL-P1-41, 3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1^SKP2 Inhibitor III

Primary Target: Skp2

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概述

Replacement Information

重要规格表

Empirical Formula
C₂₄H₂₄N₂O₃S

价格及供货情况

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Description
Overview	A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination, effectively preventing Skp2 substrates activation (Akt) and degradation (p21 & p27) with concomitant down-regulation of cellular Skp2 protein level (10 to 20 µM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC₅₀ from 1.22 to 10.5 µM) and reduces ALDH⁺ cancer stem cell population in PC3 cultures (10 to 20 µM). Exhibits good pharmacokinetic property and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80 mg/kg/d i.p.) in vivo.
Catalogue Number	506305
Brand Family	Calbiochem®
Synonyms	p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCF^SKP2 Inhibitor III, SZL-P1-41, 3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1^SKP2 Inhibitor III

References
References	Chan, C.H., et al. 2013 Cell 154, 556.

Product Information
Form	Beige powder
Hill Formula	C₂₄H₂₄N₂O₃S
Chemical formula	C₂₄H₂₄N₂O₃S
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	Skp2
Purity	≥98% 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
5.06305.0001	04055977243246

Documentation

SKP2 E3 Ligase Inhibitor III - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Chan, C.H., et al. 2013 Cell 154, 556.

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	15-January-2013 JSW
Synonyms	p27/Kip1 Activator III, S-phase Kinase-associated Protein 2 Inhibitor III, SCF^SKP2 Inhibitor III, SZL-P1-41, 3-(1,3-Benzothiazol-2-yl)-6-ethyl-7-hydroxy-8-(1-piperidinylmethyl)-4H-chromen-4-one, 3-(Benzo[d]thiazol-2-yl)-6-ethyl-7-hydroxy-8-(piperidin-1-ylmethyl)-4H-chromen-4-one, 3-Benzothiazol-2-yl-6-ethyl-7-hydroxy-8-(piperidylmethyl)chromen-4-one, p21/Cip1/CKI/Waf1 Activator III, CRL1^SKP2 Inhibitor III
Description	A cell-permeable benzothiazolylchromenone compound that disrupts Skp2-Skp1 interaction via direct Skp2 affinity binding and selectively prevents Skp2-, but not Fbw7- or β-TrCP-, Skp1-Cullin-1-F-box (SFC) complex-mediated substrates ubiquitination both in cell-free systems and in cultures, effectively preventing ubiquitination-dependent activation (Akt) and degradation (p21 & p27) of Skp2 substrates with concomitant down-regulation of cellular Skp2 protein level (10 to 20 µM in HEK293T & PC3 cultures). Exhibits antiproliferation activity toward a panel of 8 cancer (IC₅₀ from 1.22 to 10.5 µM), but not normal PNT1A epithelial or IMR90 fibroblast, lines and effectively reduces ALDH⁺ cancer stem cell (CSC; Cancer Initiating Cell) population in prostate cancer PC3 cultures (10 to 20 µM) by promoting p53-independent senescence and blocking Akt-dependent aerobic glycolysis. Exhibits good pharmacokinetic property (t_max = 1 h; t_1/2 >6 h; C_max >1 µM/plasma and >4 µM/tumor in 200 mm³ PC3 tumor-bearing mice; 80 mg/kg i.p.) and is efficacious in suppressing A549 and PC3 tumor growth in mice (40 to 80 mg/kg/d i.p.) in vivo.
Form	Beige powder
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₂₄H₂₄N₂O₃S
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (5 mg/ml). Use only fresh DMSO for reconstitution.
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	Chan, C.H., et al. 2013 Cell 154, 556.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Proteases Inhibitors > Proteasome and Ubiquitination Pathway Inhibitors

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