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XMU-MP-1

CAS号

2061980-01-4

分子式

C17H16N6O3S2

主要靶点

Hippo pathway

仅限科研使用

Cat No : CM05215

Print datasheet

Synonyms

Hippopathway|Hippo pathway|Hippo (MST)|inhibit|Inhibitor|MST1|MST2|XMUMP1|XMU-MP-1|XMU MP 1

验证数据展示

  • CAS No.: 2061980-01-4

    XMU-MP-1
    CAS#: 2061980-01-4

产品信息

CAS号 2061980-01-4
分子式 C17H16N6O3S2
主要靶点 Hippo pathway
主要通路 干细胞
分子量 416.48
纯度 99.68%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Hippopathway|Hippo pathway|Hippo (MST)|inhibit|Inhibitor|MST1|MST2|XMUMP1|XMU-MP-1|XMU MP 1

靶点活性

MST1:71.1 nM|MST2:38.1 nM

体内活性

XMU-MP-1在体内药代动力学表现出色，能够通过1至3mg/kg的剂量腹腔注射，显著增强小鼠在急性及慢性肝损伤模型中的肠道修复、肝脏修复和再生能力。XMU-MP-1治疗在Fah缺陷小鼠模型中显示出比车辆对照组更高的人类肝细胞重新填充率，表明XMU-MP-1治疗可能促进人类肝脏再生。因此，通过药理调节MST1/2激酶活性，提供了一种新的增强组织修复和再生的方法，XMU-MP-1作为开发针对性再生治疗药物的先导化合物。

体外活性

XMU-MP-1在0.1至10μM的浓度范围内，以剂量依赖的方式降低了HepG2细胞内内源性MOB1, LATS1/2及YAP的磷酸化水平。此外，XMU-MP-1处理抑制了在包括鼠巨噬细胞样细胞、人成骨肉瘤细胞、人结直肠腺癌细胞等多种细胞系中由过氧化氢激发的MOB1磷酸化以及MST1/2的自磷酸化。XMU-MP-1阻断了MST1/2的激酶活性，从而激活了下游效应蛋白Yes-associated protein，促进细胞生长。XMU-MP-1能够强效且可逆地抑制MST1/2激酶的活性，并在细胞中增强其下游的YAP激活。

溶解度

DMSO:12.5 mg/mL (30.01 mM)

参考文献

1.Fan F, et al. Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci Transl Med. 2016 Aug 17;8(352):352ra108.
2.Zhu Y, Gu H, Yang L, et al. The sequential role of Mst1/mTORC1/STAT1 activity in chemokine receptor 2-regulated B cell receptor signaling[J]. Authorea Preprints. 2021
3.Shang Y, Yan Y, Chen B, et al. Over‐expressed MST1 impaired spatial memory via disturbing neural oscillation patterns in mice[J]. Genes, Brain and Behavior. 2020: e12678.
4.Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation[J]. Cell Death & Differentiation. 2021: 1-18.

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