化合物 LDN-193189|T1935

價(jià)格	￥398	￥578	￥788
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱(chēng):化合物 LDN-193189	英文名稱(chēng):LDN193189
CAS:1062368-24-4	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.86%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T1935

Product Introduction

Bioactivity

名稱(chēng)	LDN193189
描述	LDN193189 (DM-3189) is a selective inhibitor of the BMP type I receptor that inhibits ALK2 and ALK3 (IC50=5/30 nM), with less activity against ALK4, ALK5, and ALK7. LDN193189 can be used in studies of progressive ossifying fibrous dysplasia.
細(xì)胞實(shí)驗(yàn)	C2C12 cells were seeded into 96-well plates at 2,000 cells per well in DMEM supplemented with 2% FBS. We treated the wells in quadruplicate with BMP ligands and LDN-193189 or vehicle. We collected the cells after 6 d in culture in 50 μl Tris-buffered saline and 1% Triton X-100. We added the lysates to p-nitro-phenylphosphate reagent in 96-well plates for 1 h and then evaluated alkaline phosphatase activity (absorbance at 405 nm). We measured cell viability and quantity by Cell Titer Aqueous One (absorbance at 490 nm), using replicate wells treated identically to those used for alkaline phosphatase measurements [1].
動(dòng)物實(shí)驗(yàn)	In the first experiment, SCID mice were implanted with MDA-PCa-118b tumors. After 7 days when tumors reached measurable sizes, mice were injected with LDN-193189 (3 mg/kg) or with vehicle intraperitoneally twice a day. Tumor sizes and body weights were measured weekly. Mice were injected with calcein at three days and one day prior to sacrifice. Blood was collected and tumors were weighed. A portion of the tumors were fixed in formaldehyde for micro-computed tomography, using EVS CT, or further decalcified for bone histomorphometric analysis, using the OsteoMeasure Analysis System, or flash frozen for RNA preparation. Osteocalcin in the mouse serum was determined by ELISA. In the second experiment, PCa-118b tumors were first digested with Accumax, and the isolated cells were plated overnight, digested by Accutase, resuspended in Matrigel in 1:1 ratio, and injected into SCID mice (1 × 10^6 cells/mouse) subcutaneously. Mice were treated with LDN-193189 five days post-injection [3].
體外活性	方法：肺動(dòng)脈平滑肌細(xì)胞 PASMCs 用 LDN193189 (2-32000 nM) 預(yù)處理 10 min，再用 BMP4 (10 ng/mL) 或 TGF-β (0.5 ng/mL) 處理 30 min，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：用 LDN193189 處理的 PASMC 的顯示對(duì) BMP4 或 TGF-β 信號(hào)傳導(dǎo)的不同抑制，IC50 分別為 5 nM 和 ≥1 μM。[1] 方法：未分化的 C2C12 細(xì)胞用 Smad3/4 反應(yīng)性 (CAGA)12-熒光素酶或 Smad1/5 反應(yīng)性 BRE 熒光素酶報(bào)道基因構(gòu)建體連同組成型表達(dá)的海腎熒光素酶轉(zhuǎn)染過(guò)夜。細(xì)胞被血清饑餓，并用 LDN193189 (0.05-5 μM) 和 GDF8、TGF-β 或 BMP2 處理 6 h，檢測(cè)熒光素酶活性。結(jié)果：LDN193189 從 0.05 μM 抑制 GDF8 誘導(dǎo)的 (CAGA)12-熒光素酶活性。0.05 μM 的 LDN193189 可有效抑制 BMP2 誘導(dǎo)的 BRE 熒光素酶活性。TGF-β誘導(dǎo)的 (CAGA)12-熒光素酶活性被 0.5 μM 的 LDN193189 抑制。[2]
體內(nèi)活性	方法：為研究 ALK2 激酶抑制對(duì)體內(nèi)異位鈣化的影響，將 LDN193189 (3 mg/kg) 腹腔注射給 caALK2 轉(zhuǎn)基因和野生型小鼠，每 12 h 一次，持續(xù) 60 天。結(jié)果：在 P30 時(shí)，LDN193189 在大約三分之二的小鼠中預(yù)防了異位骨，并減輕了其余小鼠的損傷。而在 P60 時(shí)，LDN193189 在三分之一的小鼠中防止了異位骨并減輕了剩余小鼠的損傷。[1]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : Insoluble DMSO : 1.45 mg/mL (3.56 mM), when pH is adjusted to 2 with HCl. Sonication is recommended. 0.01M HCL : 1.67 mg/mL (4.1 mM）
關(guān)鍵字	Inhibitor \| Transforming growth factor beta receptors \| inhibit \| DM3189 \| LDN193189 \| DM 3189 \| TGF-β Receptor
相關(guān)產(chǎn)品	Monocrotaline \| Pirfenidone \| Ceritinib \| A 83-01 \| Chromenone 1 \| LY-364947 \| BMP signaling agonist sb4 \| Alectinib hydrochloride \| SB-431542 \| Galunisertib \| Alantolactone \| Hydrochlorothiazide

關(guān)鍵字： LDN-193189|||LDN 193189|||DM-3189|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專(zhuān)業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷(xiāo)售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類(lèi)企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類(lèi)型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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