NSC 23766 trihydrochloride

目錄號：S8031 Purity: 99.96%

NSC 23766 trihydrochloride是一種Rac GTPase抑制劑，通過鳥嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化，無細胞試驗中IC50為~50 μM；但是不會抑制密切相關(guān)的靶點，Cdc42或RhoA。

NSC 23766 trihydrochloride Chemical Structure

CAS: 1177865-17-6

規(guī)格	價格	庫存
10mM (1mL in DMSO)	1139.63	現(xiàn)貨
10mg	901.16	現(xiàn)貨
50mg	3849.78	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.96%

99.96

NSC 23766 trihydrochloride相關(guān)產(chǎn)品

相關(guān)靶點	Cdc42-subclass Rac Rho-subclass	點擊展開
相關(guān)產(chǎn)品	EHop-016 CCG-1423 ML141 EHT 1864 2HCl ZCL278 MBQ-167 CCG-203971 Rhosin hydrochloride CID44216842	點擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息(PMID)
A431	Growth Inhibition Assay	100 μM	24/48/72 h	inhibits cell growth in a time dependent manner	25109327
RBMECs	Function Assay	100 μM?	30?min	blockes 6Bnz-cAMP-mediated activation of Rac1 in EMAP-II-treated RBMECs	26358039
U2-OS	Growth Inhibition Assay	100 μM	24/48/72 h	inhibits cell growth in a time dependent manner	25109327
SW480?	Growth Inhibition Assay	100 μM	24/48/72 h	inhibits cell growth in a time dependent manner	25109327
A431	Function Assay	100 μM	24 h	induces cell cycle arrest in the G1 phase?	25109327
U2-OS	Function Assay	100 μM	24 h	induces cell cycle arrest in the G1 phase?	25109327
SW480?	Function Assay	100 μM	24 h	induces cell cycle arrest in the G1 phase?	25109327
Ki-67+?CLL	Growth Inhibition Assay	50 μM	5 d	decreases the number of Ki-67+?CLL cells	24501217
NIH3T3?	Growth Inhibition Assay	100 μM	24?h	has no significant impact on cell viability	25037060
U87MG	Cell Viability Assay	50 mM	144 h	exhibits synergistic antiproliferative effects combined treatment with erlotinib?	23832120
A172MG	Cell Viability Assay	50 mM	144 h	exhibits synergistic antiproliferative effects combined treatment with erlotinib?	23832120
T98MG	Cell Viability Assay	50 mM	144 h	exhibits synergistic antiproliferative effects combined treatment with erlotinib?	23832120
PC38	Cell Viability Assay	50 mM	144 h	exhibits synergistic antiproliferative effects combined treatment with erlotinib?	23832120
U87MG	Function Assay	50 mM	24 h	enhances the antimigratory effect of erlotinib	23832120
PC40	Cell Viability Assay	50 mM	144 h	exhibits synergistic antiproliferative effects combined treatment with erlotinib?	23832120
T98MG	Function Assay	50 mM	24 h	enhances the antimigratory effect of erlotinib	23832120
A172MG	Function Assay	50 mM	24 h	enhances the antimigratory effect of erlotinib	23832120
NCI-H1703	Growth Inhibition Assay	0-500 μM	24 h	inhibits cell growth in a dose dependent manner	22549160
NCI-H1703	Function Assay	100 μg/ml	24 h	slows progression through the G1?phase of the cell cycle	22549160
NCI-H1703	Function Assay	0-500 μM	24 h	diminishes basal NF-κB activity dose dependently?	22549160
SKBR3	Function Assay	50 μM	24 h	inhibits Rac1 activation	21943825
SKBR3-pMKO.1	Function Assay	50 μM	24 h	inhibits Rac1 activation	21943825
MCF7	Cytotoxicity Assay	0-100 μM	48 h	decreases cell viability in a dose dependent manner	20515940
T47D	Cytotoxicity Assay	0-100 μM	48 h	decreases cell viability in a dose dependent manner	20515940
MDA-MB-468	Cytotoxicity Assay	0-100 μM	48 h	decreases cell viability in a dose dependent manner	20515940
MDA-MB-231	Cytotoxicity Assay	0-100 μM	48 h	decreases cell viability in a dose dependent manner	20515940
MDA-MB-231	Function Assay	0-100 μM	24 h	selectively inhibits Rac1 activation without interfering with the activity of the closely related small GTPase Cdc42	20515940
MDA-MB-231?	Function Assay	100 μM	48 h	increases the cell number in G1?phase and decreases the cell number in S and G2-M phases?	20515940
MCF7	Function Assay	100 μM	48 h	increases the cell number in G1?phase and decreases the cell number in S and G2-M phases?	20515940
MDA-MB-468	Apoptosis Assay	50/100 μM	24 h	induces apoptosis	20515940
T47D	Function Assay	100 μM	48 h	increases the cell number in G1?phase and decreases the cell number in S and G2-M phases?	20515940
MDA-MB-468	Function Assay	100 μM	24 h	inhibits?caspase-3 activation?	20515940
MDA-MB-468	Function Assay	50/100 μM	24 h	increases phosphorylation of JNK in a dose dependent manner	20515940
MDA-MB-231?	Function Assay	50/100 μM	24 h	increases phosphorylation of JNK in a dose dependent manner	20515940
MDA-MB-468	Function Assay	50/100 μM	48 h	induces a dose-dependent decrease in phosphorylation of p65 subunit	20515940
MDA-MB-231?	Function Assay	50/100 μM	48 h	induces a dose-dependent decrease in phosphorylation of p65 subunit	20515940
IEC-6?	Function Assay	120 μM	4/6/8 h	prevents the increased activation of FAK at 6 and 8 h	20448461
RA1	Function Assay	50 μM	24 h	inhibits Matrigel invasion	17622308
RA-FLS (RA2)?	Growth Inhibition Assay	25/50 μM	1-9 d	inhibits cell growth in both dose and time dependent manner	17622308
RA2	Function Assay	50 μM	24 h	inhibits Matrigel invasion	17622308
RA4	Function Assay	50 μM	24 h	inhibits Matrigel invasion	17622308
RA3	Function Assay	50 μM	24 h	inhibits Matrigel invasion	17622308
human aortic smooth muscle cells	Function Assay	50 uM		Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence	19527032
human aortic smooth muscle cells	Function Assay	100 μM		Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 100 uM by SDS-PAGE based chemiluminescence	19527032
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生物活性

產(chǎn)品描述

靶點

Rac GTPase ^[1]
(Cell-free assay)

50 μM


體外研究(In Vitro)
體外研究活性	NSC23766被認為可以融入Rac1的表面溝槽，Rac1對GEF規(guī)格至關(guān)重要。NSC23766通過Rac特異性的GEF Trio或 Tiam1，有效地抑制Rac1結(jié)合和激活，這種作用具有劑量依賴性，通過其各自的GEFs，不干擾緊密相關(guān)的Cdc42或RhoA結(jié)合或激活。NSC23766有效調(diào)節(jié)細胞骨架中的Rac GTPase功能，和許多細胞功能，包括細胞周期，細胞生長，粘附，遷移和基因轉(zhuǎn)錄。NSC 23766 (50 μM)作用于NIH 3T3細胞，有效抑制血清或血小板衍生的生長因子誘導的Rac1激活和偽足形成，不影響內(nèi)源性Cdc42或RhoA活性。NSC23766降低Trio 或 Tiam1而不是Vav, Lbc, Intersectin, 和組成型激活的Rac1突變型刺激的NIH 3T3細胞生長，也抑制Trio, Tiam1,或Ras誘導的細胞轉(zhuǎn)化。NSC23766 抑制PC-3細胞增殖和錨定非依賴性生長，這種作用存在劑量依賴性。25 μM NSC23766抑制85%PC-3細胞侵襲穿過基底膜。^[1] 50 μM NSC 23766作用于人體血小板，抑制凝血酶誘導的Rac1和Rac2激活，以及血小板聚集。^[2] NSC23766作用于swAPP-HEK293細胞，抑制Aβ40 和 Aβ42產(chǎn)生，不影響Notch 和 sAPPα。NSC23766 抑制細胞中γ-分泌酶活性，但是不是作為直接的γ-分泌酶抑制劑。NSC23766降低分泌的和細胞內(nèi)的 Aβ40水平，IC50為48.94 μM，這種作用具有劑量依賴性。50 μM NSC 23766抑制57.97% Aβ42 釋放。^[3] NSC23766調(diào)節(jié)內(nèi)皮NO合酶表達和內(nèi)皮功能。100μM NSC23766抑制eNOS啟動子活性，牛主動脈內(nèi)皮細胞中抑制60％，bEND.3細胞中抑制30％至35％。NSC23766抑制Rac1，破壞eNOS mRNA穩(wěn)定性，半衰期縮短到17小時。NSC23766 抑制ACh誘導的野生型小鼠主動脈環(huán)放松，這種作用存在劑量依賴性。^[4] NSC23766抑制細胞生長，且誘導細胞凋亡。NSC23766降低MDA-MB-468和MDA-MB-231細胞活力，這種作用存在劑量依賴性， IC50 為~10 μM,與雌激素受體（ER），孕酮受體（PR），Her2，和p53基因突變狀態(tài)無關(guān)。NSC23766對MCF12A正常乳腺上皮細胞的存活幾乎沒有影響。NSC 23766處理MDA-MB-231細胞24小時后，G1期細胞增長41％至65％，S和G2-M期隨之減少。100 μM NSC23766誘導MDA-MB-468細胞凋亡增長6倍。NSC23766作用于乳腺癌細胞，抑制細胞周期停滯或凋亡，通過下調(diào)cyclin D1, survivin, X-連鎖蛋白凋亡抑制劑（XIAP）而調(diào)節(jié)。^[5]
激酶實驗	Rho GTPase活性測定
激酶實驗	10-cm培養(yǎng)皿中的對數(shù)生長期細胞生長在0.5％血清培養(yǎng)基中饑餓處理24小時，然后溶解在含20 mM Tris HCl (pH 7.6), 100 mM NaCl, 10 mM MgCl₂, 1% Nonidet P-40, 10% 甘油, 和1×蛋白酶抑制劑混合物的Buffer中。澄清裂解液，蛋白濃度歸一化，通過效應(yīng)結(jié)構(gòu)域下拉檢測測量裂解液中與GTP結(jié)合的Rac1。His6-PAK1 PBD拉下實驗中，E. coli純化的Ni²⁺-瓊脂糖固定的His6-PAK1 PBD域與細胞裂解液溫育30分鐘。使用anti-Rac1單克隆抗體，通過免疫印跡，在洗滌緩沖液中洗滌兩次Ni²⁺瓊脂糖共同沉淀。
細胞實驗	細胞系	人類乳腺癌細胞 MDA-MB-468
	濃度	0-100 μM
	孵育時間	2 天
	方法	細胞按1.5×10⁴個/mL接種在96孔組織培養(yǎng)板中，孔中含200 μL培養(yǎng)基。接種24小時后, 使用含指定濃度NSC23766的 200 μL新鮮培養(yǎng)基置換原來的培養(yǎng)基。處理末期，每孔加入20 μL MTS 溶液，在37°C下溫育2小時。在96孔板酶標儀上讀取490 nm處吸光值。
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Western blot	pCREB / CREB OCT4 / SOX2 / Nanog active Rac1 / Rac1		25319697
	Immunofluorescence

NSC 23766 trihydrochloride

產(chǎn)品質(zhì)控

NSC 23766 trihydrochloride相關(guān)產(chǎn)品

相關(guān)信號通路圖

細胞實驗數(shù)據(jù)示例

生物活性