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LY-364947

CAS号

396129-53-6

分子式

C17H12N4

主要靶点

MLK|Casein Kinase|RIP kinase|TGF-beta/Smad

仅限科研使用

Cat No : CM06629

Print datasheet

Synonyms

CaseinKinase|Casein Kinase|CK1δ|inhibit|HTS466284|HTS-466284|HTS 466284|Smad|TGFb|TGF-b/Smad|TGFβRI|TGFβRII|TGFβ|TGF-β Receptor|TGF-β/Smad|TGFbeta|TGF-beta|TGFbeta/Smad|Transforming growth factor beta receptors|RIP kinase|RIPK2|RIPkinase|Inhibitor|MLK-7K|LY364947|LY-364947|LY 364947

验证数据展示

  • CAS No.: 396129-53-6

    LY-364947
    CAS#: 396129-53-6

产品信息

CAS号 396129-53-6
分子式 C17H12N4
主要靶点 MLK|Casein Kinase|RIP kinase|TGF-beta/Smad
主要通路 干细胞|NF-κB 信号通路|凋亡|干细胞|代谢|MAPK 信号通路
分子量 272.3
纯度 99.96%， 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 CaseinKinase|Casein Kinase|CK1δ|inhibit|HTS466284|HTS-466284|HTS 466284|Smad|TGFb|TGF-b/Smad|TGFβRI|TGFβRII|TGFβ|TGF-β Receptor|TGF-β/Smad|TGFbeta|TGF-beta|TGFbeta/Smad|Transforming growth factor beta receptors|RIP kinase|RIPK2|RIPkinase|Inhibitor|MLK-7K|LY364947|LY-364947|LY 364947

靶点活性

TGFβRII:0.4 μM|CK1δ:0.22 μM|RIPK2:0.11 μM|TGFβRI:59 nM|MLK7K:1.4 μM

体内活性

在浓度低至0.25 μM时,LY364947使NMuMg细胞中的xVent2-lux BMP4响应增强30％。2 μM LY364947防止NMuMg细胞中TGF-β诱导的上皮 - 间质转化。3 μM LY364947处理24小时后,几乎在所有HDLECs中诱导Prox1和LYVE-1表达。LY364947促进Foxo3a的核输出,在白血病阳性细胞中具有低Smad2/3和高Akt磷酸化水平。 与OP-9基质细胞共培养后,LY364947（<20 μM）抑制白血病起始细胞集落形成能力。LY364947作为一种ATP竞争性,紧密结合抑制剂,通过TGFβR-I激酶抑制P-Smad3磷酸化,Ki为28 nM。LY364947抑制体内Smad2磷酸化,NMuMg细胞中IC50为135 nM。LY364947抑制NMuMg细胞内的体内Smad2磷酸化,IC50为135 nM。

体外活性

1 mg/kg i.p. LY364947在BxPC3胰腺癌细胞的肿瘤异种移植模型中,明显增加肿瘤组织中LYVE-1-阳性区域.25 mg/kg i.p. LY364947在慢性腹膜炎小鼠模型中,明显增加的LYVE-1-阳性区域表明其加速淋巴管生成.Y364947（25 mg/kg）可增加CML感染小鼠中白血病起始细胞中的p-Akt和减少核Foxo3a.

溶解度

DMSO:7.5 mg/mL (27.54 mM)

参考文献

1.Li HY, et al. J Med Chem, 2006, 49(6), 2138-2142.
2.Vogt J, et al. Cell Signal, 2011, 23(11), 1831-1842.
3.Peng SB, et al. Biochemistry, 2005, 44(7), 2293-2304.
4.Oka M, et al. Blood, 2008, 111(9), 4571-4579.
5.Naka K, et al. Nature, 2010, 463(7281), 676-680.
6.Deng Y, Li L, Zhu J H, et al. COX-2 promotes the osteogenic potential of BMP9 through TGF-β1/p38 signaling in mesenchymal stem cells[J]. Aging (Albany NY) . 2021, 13(8): 11336.
7.Chen Q Z, Li Y, Shao Y, et al. TGF-β1/PTEN/PI3K signaling plays a critical role in the anti-proliferation effect of tetrandrine in human colon cancer cells [J]. International journal of oncology. 2017, 50(3): 1011-1021.
8.Li Q, Ma Y, Liu X L, et al. Anti?proliferative effect of honokiol on SW620 cells through upregulating BMP7 expression via the TGF?β1/p53 signaling pathway[J]. Oncology Reports. 2020

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