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- 2x SYBR Green qPCR Master Mix
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- 2x SYBR Green qPCR Master Mix(High ROX)
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- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
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GW3965 HCl
GW3965 HCl是一種有效的，選擇性LXR激動(dòng)劑，作用于hLXRα和hLXRβ，無細(xì)胞試驗(yàn)中EC50分別為190和30 nM。
GW3965 HCl Chemical Structure
CAS: 405911-17-3
產(chǎn)品質(zhì)控
批次：
純度：
99.88%
99.88
常與GW3965 HCl一起在實(shí)驗(yàn)中被使用的化合物
在MAS98.12模型中，GW3965和Carboplatin比單獨(dú)Carboplatin顯著減小相對(duì)腫瘤體積。
GW3965和Pioglitazone組合預(yù)處理原代小膠質(zhì)細(xì)胞可導(dǎo)致iNOS轉(zhuǎn)錄物顯著減少。
Skerrett R, et al. J Biol Chem. 2015 Aug 28;290(35):21591-602.
GW3965HCl和Bexarotene誘導(dǎo)急性髓系白血病(AML)細(xì)胞的分化和凋亡。
GW3965可以增加Gefitinib誘導(dǎo)的HCC827/GR-8-2細(xì)胞系細(xì)胞凋亡和細(xì)胞周期停滯。
在A375異種移植模型中，GW3965和Navitoclax(ABT-263)聯(lián)合治療比單獨(dú)使用任一藥物更能明顯抑制腫瘤生長(zhǎng)。
GW3965 HCl相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | LXR-α LXR-β | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | T0901317 LXR-623 SR9243 AZ876 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫(kù) | 代謝化合物庫(kù) 抗癌代謝化合物庫(kù) 谷氨酰胺代謝化合物庫(kù) 糖代謝化合物庫(kù) 脂代謝化合物庫(kù) | 點(diǎn)擊展開 |
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| HEK293 | 10 uM | 20 hrs | Activation of rat LXRbeta expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay | 28006909 | |
| HEK293 | 10 uM | 20 hrs | Activation of human LXRalpha expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay | 28006909 | |
| HepG2 | Function assay | 500 nM | Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced srebp1c mRNA expression in human HepG2 cells at 500 nM | 18800767 | |
| HepG2 | Function assay | 500 nM | Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced fas mRNA expression in human HepG2 cells at 500 nM | 18800767 | |
| RAW264.7 | Function assay | 1 uM | Reduction of LPS-stimulated iNOS gene expression in mouse RAW264.7 cells expressing LXRalpha at 1 uM by luciferase reporter gene assay | 18800767 | |
| RAW264.7 | Function assay | 1 uM | Inhibition of LPS-stimulated nuclear co-repressor release from iNOS promoter in mouse RAW264.7 cells at 1 uM by RT-PCR | 18800767 | |
| HeLa | Function assay | 1 uM | Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis | 18800767 | |
| HeLa | Function assay | 1 uM | Induction of LXRbeta SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis | 18800767 | |
| HeLa | Function assay | 1 uM | Induction of LXRalpha SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis | 18800767 | |
| THP1 | Antiinflammatory assay | 6 hrs | Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA, IC50 = 0.02 μM. | 18800767 | |
| COS7 | Function assay | 16 hrs | Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay, EC50 = 0.015 μM. | 17587573 | |
| THP1 | Function assay | 18 hrs | Induction of cholesterol efflux in THP1 cells after 18 hrs, EC50 = 0.01 μM. | 17416521 | |
| RAW264.7 | Function assay | 24 hrs | Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs, EC50 = 0.029 μM. | 19717304 | |
| SH-SY5Y | Function assay | 24 hrs | Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50 = 0.13 μM. | 19264481 | |
| SH-SY5Y | Function assay | 24 hrs | Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50 = 0.31 μM. | 19264481 | |
| CHOK1 | Function assay | 24 hrs | Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.42 μM. | 25677664 | |
| CHOK1 | Function assay | 24 hrs | Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50 = 1.3 μM. | 25677664 | |
| THP1 | Function assay | Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay, EC50 = 0.027 μM. | 17665897 | ||
| COS7 | Function assay | Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay, EC50 = 0.015 μM. | 17416521 | ||
| THP1 | Function assay | Induction of cholesterol efflux in THP1 cells, EC50 = 0.01 μM. | 17587573 | ||
| THP1 | Function assay | Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50 = 0.031 μM. | 18973288 | ||
| CV1 | Function assay | Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.03981 μM. | 20345102 | ||
| THP1 | Function assay | Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay, EC50 = 0.097 μM. | 17665897 | ||
| CV1 | Function assay | Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.1 μM. | 20345102 | ||
| HepG2 | Function assay | Effect on SREBP1c gene expression in human HepG2 cells, EC50 = 0.21 μM. | 18973288 | ||
| HuH7 | Function assay | Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.31 μM. | 18973288 | ||
| CHO | Function assay | Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50 = 0.41 μM. | 17034119 | ||
| THP1 | Function assay | Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50 = 0.434 μM. | 18973288 | ||
| CV1 | Function assay | Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.50119 μM. | 20345102 | ||
| HuH7 | Function assay | Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.66 μM. | 18973288 | ||
| CV1 | Function assay | Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.79433 μM. | 20345102 | ||
| HepG2 | Function assay | Effect on triglyceride accumulation in human HepG2 cells, EC50 = 2.002 μM. | 18973288 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | GW3965 HCl是一種有效的，選擇性LXR激動(dòng)劑，作用于hLXRα和hLXRβ，無細(xì)胞試驗(yàn)中EC50分別為190和30 nM。 | ||||||
|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | GW3965使類固醇受體共激活因子1聚集到LXRα，在無細(xì)胞配體檢測(cè)試驗(yàn)中，EC50 為125 nM。[1] GW3965對(duì)hLXRα 和 hLXRβ表現(xiàn)出有效的拮抗活性，在細(xì)胞試驗(yàn)中EC50分別為190 nM 和30 nM。此外，GW3965也對(duì)其他核受體表現(xiàn)出優(yōu)良的選擇性。[1] 在人胰島中，GW3965 (1 μM)降低選定促炎性細(xì)胞因子，包括IL-8，單核細(xì)胞趨化蛋白-1和組織因子的表達(dá)。[4] |
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|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | Skp2 / pEGFR / EGFR / pERK / ERK LXRα / LXRβ / ABCA1 / ABCG1 |
|
25184494 | |
| Immunofluorescence | LAMP-1 / LDLR pRelA |
|
23382078 | |
| Growth inhibition assay | Cell viability |
|
25184494 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在小鼠體內(nèi)，GW3965在10 mg/kg劑量下使ABCA1表達(dá)上調(diào)8倍，并使循環(huán)水平提高30%，Cmax為12.7 μg/mL ，t1/2為2小時(shí)。[1] 在LDLR−/−和apoE−/−小鼠體內(nèi)，GW3965 (10mg/kg)誘導(dǎo)ABCA1 和ABCG1表達(dá)，并表現(xiàn)出有效的抗動(dòng)脈粥樣硬化活性。[2] 在雄性sprague-dawley大鼠體內(nèi)，GW3965降低Ang II介導(dǎo)的血壓增加，并減少血管Ang II受體基因表達(dá)。[3] 在惡性膠質(zhì)瘤小鼠模型中，GW3965導(dǎo)致LDLR降解，增加ABCA1膽固醇外排轉(zhuǎn)運(yùn)體的表達(dá)，從而有效促進(jìn)腫瘤細(xì)胞死亡。[5] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | C57BL/6 小鼠 |
| Dosages | ≤10 mg/kg | |
| Administration | 口服 | |
化學(xué)信息&溶解度
| 分子量 | 618.51 | 分子式 | C33H31ClF3NO3.HCl |
| CAS號(hào) | 405911-17-3 | SDF | Download GW3965 HCl SDF |
| Smiles | C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (161.67 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
How to formulate the compound for mouse in vivo experiment?
回答：
S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.
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