|(E)-3-(对甲苯磺酰基)丙烯腈|CsnPharm

CAS No.: 19542-67-7

(E)-3-Tosylacrylonitrile Catalog No. CSN13487

Synonyms: (E)-3-Tosylacrylonitrile

BAY 11-7082 is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. It also inhibits components of the ubiquitin system through inactivating the E2-conjugating enzymes Ubc (ubiquitin conjugating) 13 and UbcH7 and the E3 ligase LUBAC (linear ubiquitin assembly complex).

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实验方案

技术信息

生物活性

描述The NF-kB pathway plays a key role in multiple cellular processes, including immune signaling, inflammation, development, proliferation and survival. NF-κB suppression occurred through inhibition, activation, phosphorylation and degradation of IκB-α, p65 phosphorylation, p65 nuclear translocation, and NF-κB-mediated reporter gene transcription. BAY 11-7082 is an IκB-α inhibitor with IC50 value of ~10μM for inhibiting the TNF-α-induced loss of IκB-α in HUVEC cells. Pre-treatment with BAY 11-7082 at concentration ranging in 1-20μM for 1h dose-dependently led to stabilization of p-IκB-α and suppression of activation of NF-κB induced by TNF-α in HUVEC cells, but no effect on constitutive phosphorylation of IκB-α. 5μM BAY 11-7082 could rapidly reduce the DNA binding of NF-κB in HTLV-I–infected T-cell through inhibition of IκB-α, resulting in downregulation of NF-κB-targeted antiapoptotic gene Bcl-xL, thus it induced apoptosis of HTLV-I–infected T-cell lines. Intraperitoneal injection with BAY 11-7082 at dose of 5mg/kg twice weekly for 28 days led to modest overall reduction in tumor volumes in HT-29 colon cancer xenografts, but showed more potency to prevent readhesion or seeding of intra-abdominal tissues through administration for 21 days in HCT-116 colon cancer xenografts. Bay 11-7082 potently inhibited GSDMD pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. It covalently modify a conserved Cys (Cys191 in human and Cys192 in mouse GSDMD) that is critical for pore formation.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A549	10 µM	Function Assay	12 h	suppresses Dvl-3 induced activation of p65	25156800
A549	10 μM	Function Assay	1 h	inhibits the increase of phospho-IκBα in PA103-infected cultures	24612488
A549	1 μM	Function Assay	48 h	enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation	23900080

更多
动物研究
剂量
Mice: 10 mg/kg^[5] (i.v.); min = 5 mg/kg^[6], max = 20 mg/kg^[7] (i.p.)

给药途径
i.v., i.p.
参考文献

动物研究
剂量	Mice: 10 mg/kg^[5] (i.v.); min = 5 mg/kg^[6], max = 20 mg/kg^[7] (i.p.)
给药途径	i.v., i.p.

[1] Pierce JW, Schoenleber R, Jesmok G, et al. Novel inhibitors of cytokine-induced IkappaBalpha phosphorylation and endothelial cell adhesion molecule expression show anti-inflammatory effects in vivo. J Biol Chem. 1997;272(34):21096-103
[2] Mori N, Yamada Y, Ikeda S, et al. Bay 11-7082 inhibits transcription factor NF-kappaB and induces apoptosis of HTLV-I-infected T-cell lines and primary adult T-cell leukemia cells. Blood. 2002;100(5):1828-34
[3] Scaife CL, Kuang J, Wills JC, et al. Nuclear factor kappaB inhibitors induce adhesion-dependent colon cancer apoptosis: implications for metastasis. Cancer Res. 2002;62(23):6870-8
[4] Identification of pyroptosis inhibitors that target a reactive cysteine in gasdermin D

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.8251 mL
- 24.1255 mL
- 48.2509 mL
- 5 mM
- 0.9650 mL
- 4.8251 mL
- 9.6502 mL
- 10 mM
- 0.4825 mL
- 2.4125 mL
- 4.8251 mL

技术信息

CAS号

19542-67-7

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C10H9NO2S

运输

蓝冰

分子量

207.25

别名

(E)-3-Tosylacrylonitrile

溶解度

DMSO	200.0 mg/mL (965.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	60 mg/mL	suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

A549	10 µM	Function Assay	12 h	suppresses Dvl-3 induced activation of p65	25156800
A549	10 μM	Function Assay	1 h	inhibits the increase of phospho-IκBα in PA103-infected cultures	24612488
A549	1 μM	Function Assay	48 h	enhances the up-regulation of IκB and subsequent decrease in Bax expression induced by combined stimulation	23900080
A549	1 μM	Apoptosis Assay	48 h	reduces the cell death induced by combined stimulation	23900080
A549	-	Function Assay	1 h	inhibits LTA-induced SP-A mRNA production significantly	23031213
A-549	10 μM	Growth Inhibition Assay	24/48 h	inhibits cell growth in a time-dependent manner	20866043
A549RT-eto	10 μM	Apoptosis Assay	24 h	accelerates FERO-mediated apoptosis	24535083
A549RT-eto	10 μM	Apoptosis Assay	24 h	accelerates F14 extract-mediated apoptosis combined treatment with F14	24220725
A549RT-eto	10 μM	Function Assay	24 h	decreases the expression levels of NF-κB and P-gp	24220725
AGS	10/20/30 μM	Growth Inhibition Assay	6/24 h	suppresses cell viability significantly	23846545
AM	5 µM	Growth Inhibition Assay	4/8 d	reduces the viability of intracellular MTB	23634218
AP	5/10 μM	Function Assay	48 h	downregulates the BAD protein level a dose-dependent manner	20596645
AP	20 μM	Function Assay	4/8 h	downregulates the BAD protein level a time-dependent manner	20596645
AQ1	5/10 μM	Function Assay	48 h	downregulates the BAD protein level a dose-dependent manner	20596645
AQ1	20 μM	Function Assay	4/8 h	downregulates the BAD protein level a time-dependent manner	20596645
ARPE-19	1 μM	Function Assay	0.5 h	suppresses TG-induced IL-8 promoter activation	25593029
BAFs	0.5/1 μM	Function Assay	24 h	inhibits TNFα/DEX induced CYP19A1 transcripts	23485457
Ca9–22	10 μM	Apoptosis Assay	1 h	completely inhibits ALA-PDT-induced apoptosis	21138480
Ca9–22	10 μM	Function Assay	1 h	completely abrogates the ALA-PDT-induced JNK activation	21138480
DSCs	2.5 μM	Function Assay	0.5 h	reverses the enhancement of CCL2/CCR2 expression of DSCs induced by IL-33	24344240
FaDu	-	Function Assay	2 h	inhibits p65 expression and blocks TNFα-induced TWIST expression	24220622
HaCaT	5.0 μM	Function Assay	1 h	attenuates the TCOH-induced production of IL-6	23041168
HBE	10μM	Function Assay	3h	abolishes the increases of IL-6 expression induced by CSE	23824089
HBL-1	3 μM	Growth Inhibition Assay	24/48/72 h	slows cell growth modestly	23441730
HBL6	0.5/5/25 μM	Apoptosis Assay	6/24 h	decreases cell viability and leeads to apoptosis in a dose-dependent manner	22074820
HCT116	5 μM	Function Assay	2 h	attenuates silymarin-induced downregulation of cyclin D1	25479723
HeLa	10 μM	Function Assay	1.5 h	abolishes BPA induced up regulation of FN and MMP-9	25797437
HeLa	5 μM	Function Assay	24 h	reduces the activity of TNF-α promoter	24657783
HepG2	0.3/1/3 μM	Function Assay	48 h	reduces IL6-induced PON1 expression	23791833
HGC-27	7.5/15/30 μM	Function Assay	6 h	induces the dephosphorylation and up-regulation of IκBα	23846545
HGC-27	7.5/15/30 μM	Apoptosis Assay	6 h	induces apoptosis in a time- and dose-dependent manner	23846545
HMECs	5 μM	Function Assay	2 h	abolishes TNF-α-induced VCAM-1 expression	25193116
HT29	10/30/100 μM	Function Assay	1 h	inhibites both TWEAK-induced p100 processing	23527154
HT29	10/30/100 μM	Function Assay	1 h	inhibits TNF-induced phosphorylation and degradation of IκBα	23527154
HT29	1-10 μM	Function Assay	10 h	increases HO-1 mRNA and protein expression	21620964
HUVEC	20 µM	Function Assay	0.5 h	prevents the induction of EAM expression	24551209
HUVEC	10 μM	Function Assay	0.5 h	counteractes the loss of Tie2 mRNA	23563632
HUVECs	3-30 μM	Function Assay	1 h	reduces the expression of miR-146a in a dose-dependent manner	24863965
IL-1R	2-15 μM	Function Assay	1 h	suppresses the activation of IKK family members	23441730
IL-1R	15 μM	Function Assay	1 h	suppresses the activation of and JNK	23441730
iNKT	10/100 μM	Function Assay	0.5 h	inhibits the induction of A2AR mRNA and other factor	24124453
IVD	10 μM	Function Assay	3 d	reverses TNF-α–mediated suppression of the disc matrix macromolecules aggrecan and collagen II	24176808
IVD	10 μM	Function Assay	3 d	abrogates TNF-α–induced up-regulation of ADAMTS-4 and ADAMTS-5	24176808
Jurket	2-30 μM	Growth Inhibition Assay	24 h	IC50=7.1 μM, inhibits cell growth in a dose-dependent manner	19646807
K562	2-30 μM	Growth Inhibition Assay	24 h	IC50=8 μM,inhibits cell growth in a dose-dependent manner	19646807
K562	2-20 μM	Apoptosis Assay	24 h	induces a dose-dependent apoptosis	19646807
KMS-12-BM	30 µM	Apoptosis Assay	3 h	induces MM cell death involves necrosis	23527154
macrophages	5 µM	Function Assay	3 h	partially blocks YPFS-induced expression of iNOS and COX-2	24967898
MCF-7	2.5-15 μM	Function Assay	0.5 h	causes the gradual loss of cell adhesion	23093227
MDM	5 µM	Growth Inhibition Assay	4/8 d	reduces the viability of intracellular MTB	23634218
MGC80-3	10/20/30 μM	Growth Inhibition Assay	6/24 h	suppresses cell viability significantly	23846545
MGC80-3	7.5/15/30 μM	Function Assay	6 h	induces the dephosphorylation and up-regulation of IκBα	23846545
MM.1S	30 µM	Apoptosis Assay	3 h	induces MM cell death involves necrosis	23527154
MT‐1	8 µm	Function Assay	3 h	decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐1	8 µm	Function Assay	3 h	decreases the levels of the p65 subunit of NF‐κB	23278479
MT‐2	8 µm	Function Assay	3 h	decreases the levels of p‐STAT3 and p‐4EBP1	23278479
MT‐2	8 µm	Function Assay	3 h	decreases the levels of the p65 subunit of NF‐κB	23278479
NCI-N87	10/20/30 μM	Growth Inhibition Assay	6/24 h	suppresses cell viability significantly	23846545
OA chondrocytes	10 μM	Function Assay	1 h	blocks the AGE-BSA-induced gene/protein expression of GRP78 or COX-2 (p<0.05)	22982228
OCM1	5 μM	Function Assay	2 h	decreases translocation of p65 in the nucleus	23443086
OCM1	2.5-20 μM	Growth Inhibition Assay	24 h	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OCM1	5 μM	Apoptosis Assay	24 h	induces apoptosis	23443086
OCM1	5 μM	Function Assay	12 h	reduces the migration	23443086
OM431	5 μM	Function Assay	2 h	decreases translocation of p65 in the nucleus	23443086
OM431	2.5-20 μM	Growth Inhibition Assay	24 h	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
OM431	5 μM	Apoptosis Assay	24 h	induces apoptosis	23443086
OM431	5 μM	Function Assay	12 h	reduces the migration	23443086
OVCXCR2	2 µM	Function Assay	48 h	blocks the CXCL1-induced cell invasion	24376747
PBMC	2-30 μM	Growth Inhibition Assay	24 h	IC50=40.2 μM, inhibits cell growth in a dose-dependent manner	19646807
PC-3	2.5/5/10 μM	Function Assay	0.5 h	blocks IGF-II-induced STS mRNA expression	24055520
RAW 264	0.2-5 µM	Function Assay	30/60/90 min	inhibits the phosphatase activity of PTP1B	23578302
RAW 264.7	5 μM	Function Assay	1 h	inhibits TNF-α and IL-12 p40 production	25019567
RAW 264.7	2-15 μM	Function Assay	1 h	suppresses the activation of IKK family members	23441730
RAW 264.7	15 μM	Function Assay	1 h	suppresses the activation of and JNK	23441730
RAW264.7	15 μM	Function Assay	15-120 min	blocks the production of NO, PGE2, and TNF-α	22745523
RAW264.7	5-30 μM	Growth Inhibition Assay	24 h	inhibits cell growth in a dose-dependent manner	22745523
SiHa	10 μM	Function Assay	1.5 h	abolishes BPA induced up regulation of FN and MMP-9	25797437
SKCXCR2	2 µM	Growth Inhibition Assay	48 h	decreases cell proliferation significantly	24376747
SKCXCR2	2 µM	Function Assay	48 h	blocks the CXCL1-induced cell invasion	24376747
SP6.5	5 μM	Function Assay	2 h	decreases translocation of p65 in the nucleus	23443086
SP6.5	2.5-20 μM	Growth Inhibition Assay	24 h	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
SP6.5	5 μM	Apoptosis Assay	24 h	induces apoptosis	23443086
SP6.5	5 μM	Function Assay	12 h	reduces the migration	23443086
THP-1	0.1/1 μM	Function Assay	0.5 h	abrogates TNF-α secretion as well as the increased secretion of IL-6 and IL-1β	24378536
THP-1	10 μM	Function Assay	1 h	abolishes the effect of rHSP27 on SR-A mRNA	23939398
THP-1	5 µM	Function Assay	1 h	inhibits MTB-induced NFκB activation	23634218
THP-1	5 µM	Growth Inhibition Assay	4/8 d	reduces the viability of intracellular MTB	23634218
THP-1	5 μM	Function Assay	0.5 h	attenuates the LPS-induced p-IκBα protein by 72%	20309718
U2OS	15 μM	Function Assay	1 h	prevents the LPS- or IL-1-stimulated formation of K63-pUb chains	23441730
U937	2-30 μM	Growth Inhibition Assay	24 h	IC50=10.5 μM, inhibits cell growth in a dose-dependent manner	19646807
VUP	5 μM	Function Assay	2 h	decreases translocation of p65 in the nucleus	23443086
VUP	2.5-20 μM	Growth Inhibition Assay	24 h	IC50=5 μM, exhibits strong anti-proliferative effects in a dose-dependent manner	23443086
VUP	5 μM	Apoptosis Assay	24 h	induces apoptosis	23443086
VUP	5 μM	Function Assay	12 h	reduces the migration	23443086
WPs	25 μM	Function Assay	5 min	suppresses ATP and vWF secretion	24331207

(E)-3-Tosylacrylonitrile Catalog No. CSN13487

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