LDN-214117 是一种 ALK2 抑制剂，具有口服活性，耐受性好，脑穿透性好。LDN-214117 对 ALK2 具有较高的选择性和较低的细胞毒性，其IC50值为 24 nM。LDN-214117 也是一种特异性的骨形态发生蛋白 (BMPs) 信号抑制剂，对 BMP6 具有相对选择的抑制作用，其IC50值为 100 nM。LDN-214117 可用于进行性骨化性纤维发育不良 (FOP) 和弥漫性内源性桥脑胶质瘤 (DIPG) 的研究。
| 生物活性 | LDN-214117 is an orally activeALK2inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity forALK2with anIC50value of 24 nM. LDN-214117 also is a specificbone morphogenetic proteins (BMPs)signaling inhibitor and has relatively selective inhibition for BMP6 with anIC50value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG)[1][2] |
| IC50& Target | IC50: 24 nM (ALK2); 27 nM (ALK1); 1,171 nM (ALK3); 3,000 nM (ALK5); 1,022 nM (BMP6); 27 nM (BMP2); 960 nM (BMP4); 16,000 nM (TGF-β1)[1] |
体外研究
(In Vitro) | LDN-214117 has high inhibition and selectivity for ALK2 kinase proteins with an IC50value of 24 nM[1].
LDN-214117 has kinase activity for ALK1, ALK3 and ALK5 with IC50values of 27 nM, 1,171 nM and 3,000 nM, respectively[1].
LDN-214117 exhibits relatively selective inhibition for BMP6, BMP2 and BMP4 with IC50values of 100 nM, 1,022 nM and 960 nM, respectively[1].
LDN-214117 has inhibition of TGF-β1-induced transcriptional activity with an IC50values of 16,000 nM[1].
LDN-214117 (5 μM, 30 min, 3 h and 24 h) has time-dependent effect activity on gene regulation level and/ or a BMP signaling pathway other than SMAD-dependent that is responsible for ID1 targeting[2].
LDN-214117 (5 μM, 24-120 h) reduces viability, proliferation and causes apoptosis of lung carcinoma cells LCLC-103H[2].
LDN-214117 (5 μM, 0-48 h) suppresses wound healing and chemotactic potential of LCLC-103H cells[2].
LDN-214117 (5 μM, 48 h) hinders growth of multicellular LCLC-103H spheroids[2].
Cell Viability Assay[2] | Cell Line: | LCLC-103H cells | | Concentration: | 5 μM | | Incubation Time: | 24 h, 48 h, 72 h and 96 h | | Result: | Decreased markedly with time, counting approximately 60% of the vehicle control level at the 96-h measurement point. |
Western Blot Analysis[2] | Cell Line: | LCLC-103H cells | | Concentration: | 5 μM | | Incubation Time: | 30 min, 3 h and 24 h | | Result: | Diminished the increase of ID1 protein. |
Apoptosis Analysis[2] | Cell Line: | LCLC-103H cells | | Concentration: | 5 μM | | Incubation Time: | 24 h, 48 h, 72 h and 96 h | | Result: | Induced considerable death of LCLC-103H cells. |
RT-PCR[2] | Cell Line: | LCLC-103H cells | | Concentration: | 5 μM | | Incubation Time: | 24 h, 48 h and 72 h | | Result: | Induced distinct gene expression patterns for the two EMTTFs. |
Cell Migration Assay[2] | Cell Line: | LCLC-103H cells | | Concentration: | 5 μM | | Incubation Time: | 0 h, 24 h and 48 h | | Result: | Significantly hindered the migration of LCLC-103H cells into the wound area by Inhibiting of BMP signaling. |
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体内研究
(In Vivo) | LDN-214117 (p.o., 25 mg/kg, daily, for 14 days) has well-tolerated in mice[3].
| Animal Model: | NOD.SCID mice[3] | | Dosage: | 25 mg/kg | | Administration: | p.o., daily, for 14 days | | Result: | Showed good-tolerated in mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 20 mg/mL(47.67 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.3837 mL | 11.9184 mL | 23.8368 mL | | 5 mM | 0.4767 mL | 2.3837 mL | 4.7674 mL | | 10 mM | 0.2384 mL | 1.1918 mL | 2.3837 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (4.77 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (4.77 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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