化合物 LDN-193189|T1935

LDN193189
1062368-24-4

￥398 1mg 起订

￥578 2mg 起订

￥788 5mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 LDN-193189

英文名称：: LDN193189

CAS号：: 1062368-24-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.86%

产品类别：: 抑制剂

货号：: T1935

Product Introduction

Bioactivity

名称	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.
细胞实验	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].
动物实验	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].
体外活性	方法：肺动脉平滑肌细胞 PASMCs 用 LDN193189 (2-32000 nM) 预处理 10 min，再用 BMP4 (10 ng/mL) 或 TGF-β (0.5 ng/mL) 处理 30 min，使用 Western Blot 检测靶点蛋白表达水平。结果：用 LDN193189 处理的 PASMC 的显示对 BMP4 或 TGF-β 信号传导的不同抑制，IC50 分别为 5 nM 和 ≥1 µM。[1] 方法：未分化的 C2C12 细胞用 Smad3/4 反应性 (CAGA)12-荧光素酶或 Smad1/5 反应性 BRE 荧光素酶报道基因构建体连同组成型表达的海肾荧光素酶转染过夜。细胞被血清饥饿，并用 LDN193189 (0.05-5 µM) 和 GDF8、TGF-β 或 BMP2 处理 6 h，检测荧光素酶活性。结果：LDN193189 从 0.05 µM 抑制 GDF8 诱导的 (CAGA)12-荧光素酶活性。0.05 µM 的 LDN193189 可有效抑制 BMP2 诱导的 BRE 荧光素酶活性。TGF-β诱导的 (CAGA)12-荧光素酶活性被 0.5 µM 的 LDN193189 抑制。[2]
体内活性	方法：为研究 ALK2 激酶抑制对体内异位钙化的影响，将 LDN193189 (3 mg/kg) 腹腔注射给 caALK2 转基因和野生型小鼠，每 12 h 一次，持续 60 天。结果：在 P30 时，LDN193189 在大约三分之二的小鼠中预防了异位骨，并减轻了其余小鼠的损伤。而在 P60 时，LDN193189 在三分之一的小鼠中防止了异位骨并减轻了剩余小鼠的损伤。[1]
存储条件	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）
关键字	Inhibitor \| Transforming growth factor beta receptors \| inhibit \| DM3189 \| LDN193189 \| DM 3189 \| TGF-β Receptor
相关产品	Monocrotaline \| Pirfenidone \| Ceritinib \| A 83-01 \| Chromenone 1 \| LY-364947 \| BMP signaling agonist sb4 \| Alectinib hydrochloride \| SB-431542 \| Galunisertib \| Alantolactone \| Hydrochlorothiazide

LDN-193189|||LDN 193189|||DM-3189|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子