文献支持LDN-212854 是一种骨形态发生蛋白 (BMP) 抑制剂，可有效抑制 ALK2 (IC50: 1.3 nM)。LDN-212854 还可抑制 ALK1 (IC50: 2.40 nM)。

价格： ￥780

品牌：medchemexpress(MCE)

货号：HY-15897

产品详情

LDN-212854 (Synonyms: 5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基)

LDN-212854 是一种骨形态发生蛋白 (BMP) 抑制剂，可有效抑制 ALK2 (IC₅₀: 1.3 nM)。LDN-212854 还可抑制 ALK1 (IC₅₀: 2.40 nM)。LDN-212854 可用于研究进行性骨化纤维发育不良和癌症，如肝细胞癌 (HCC)。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

生物活性
LDN-212854 is a bone morphogenetic protein (BMP) inhibitor that potently inhibits ALK2 (IC50: 1.3 nM). LDN-212854 also inhibits ALK1 (IC50: 2.40 nM). LDN-212854 can be used in the research of fibrodysplasia ossificans progressive and cancers, such as hepatocellular carcinoma (HCC)[1][2].

体外研究
(In Vitro)
LDN-212854 (0-3.815 μM) blocks the phosphorylation of SMAD1/5/8 induced by BMP7 in BMPR2−/− cells[1].
LDN-212854 (2.5 μM, 5 days ) inhibits cell proliferation in Huh7 and MT cells[2].
LDN-212854 (0.5 μM, 48 h ) suppresses ID1 and EpCAM expression in Huh7 and MT cells[2].

Western Blot Analysis[1]

Cell Line:   BMPR2-deficient pulmonary vascular smooth muscle cells
Concentration:   0, 1, 3, 6, 16, 39, 98, 244, 610, 1530, 3815 nM
Incubation Time:
Result:   Inhibited the phosphorylation of SMAD1/5/8 induced by BMP7 with an IC50 value of 37 nM.

体内研究
(In Vivo)
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 4 weeks) potently inhibits heterotopic ossification in an inducible transgenic mutant ALK2 mouse model of fibrodysplasia ossificans progressiva[1].
LDN-212854 (intraperitoneal injection, 6 mg/kg, twice daily for 10-14 days) suppresses HCC tumor progression through repression of ID1 in HCC xenografts model[2].

Animal Model:   Murine inducible transgenic ALK2Q207D model of heterotopic ossification[1]
Dosage:   6 mg/kg
Administration:   Intraperitoneal injection , twice daily for 4 weeks
Result:   Prevented the formation of heterotopic bone and preserved limb range of motion with minimal or no impairment in the majority of mice.

分子量
406.48

性状
Solid

Formula
C25H22N6

CAS 号
1432597-26-6

中文名称
5-（6-（4-（哌嗪-1-基）苯基）吡唑并[1,5-a]嘧啶-3-基）

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
溶解性数据
In Vitro:
DMSO : ≥ 30 mg/mL (73.80 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量   1 mg   5 mg   10 mg
1 mM   2.4601 mL   12.3007 mL   24.6015 mL
5 mM   0.4920 mL   2.4601 mL   4.9203 mL
10 mM   0.2460 mL   1.2301 mL   2.4601 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

2.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (6.15 mM); Suspended solution; Need ultrasonic

参考文献	[1]. Mohedas AH, et al. Development of an ALK2-biased BMP type I receptor kinase inhibitor. ACS Chem Biol. 2013;8(6):1291-302. [Content Brief] [2]. Han Chen, et al. BMP9-ID1 signaling promotes EpCAM-positive cancer stem cell properties in hepatocellular carcinoma. Mol Oncol. 2021 Aug;15(8):2203-2218. [Content Brief]