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(E)-N-(4-苄基-1-哌嗪基)-1-(3,5-二甲基-1-苯基-1H-吡唑-4-基)甲亚胺

用途

SANT-1 是一种有效的 Smo 拮抗剂,能够抑制 Hedgehog 通路,在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中,IC50 值分别为 20 nM 和 30 nM。

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名称

[ CAS 号 ]:
304909-07-7

[ 中文名 ]:
(E)-N-(4-苄基-1-哌嗪基)-1-(3,5-二甲基-1-苯基-1H-吡唑-4-基)甲亚胺

[ 英文名 ]:
SANT-1

[英文别名 ]:

SANT-1
Shh Signaling Antagonist V

生物活性

[ 描述 ]:

SANT-1 是一种有效的 Smo 拮抗剂,能够抑制 Hedgehog 通路,在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中,IC50 值分别为 20 nM 和 30 nM。

[ 相关类别 ]:

信号通路 >> 干细胞及 Wnt 通路 >> SMO

研究领域 >> 癌症

信号通路 >> 干细胞及 Wnt 通路 >> Hedgehog

[ 靶点 ]

IC50: 20 nM (Shh signaling), 30 nM (SmoA1)[1]

[参考文献]

[1]. Chen JK, et al. Small molecule modulation of Smoothened activity. Proc Natl Acad Sci U S A. 2002 Oct 29;99(22):14071-6.

物理化学性质

[ 密度 ]:
1.13g/cm3

[ 沸点 ]:
547.4ºC at 760mmHg

[ 熔点 ]:
104-106ºC

[ 分子式 ]:
C₂₃H₂₇N₅

[ 分子量 ]:
373.49

[ 闪点 ]:
284.8ºC

[ 精确质量 ]:
373.22700

[ PSA ]:
36.66000

[ LogP ]:
3.51660

[ 外观性状 ]:
固体;White to Orange to Green powder to crystal

[ 折射率 ]:
1.623

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
Soluble in DMSO with warming

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

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文献

Smoothened adopts multiple active and inactive conformations capable of trafficking to the primary cilium.

PLoS ONE 4(4) , e5182, (2009)

Activation of Hedgehog (Hh) signaling requires the transmembrane protein Smoothened (Smo), a member of the G-protein coupled receptor superfamily. In mammals, Smo translocates to the primary cilium up...

MicroRNA-602 and microRNA-608 regulate sonic hedgehog expression via target sites in the coding region in human chondrocytes.

Arthritis Rheumatology 67(2) , 423-34, (2015)

Hedgehog (HH) signaling has recently been associated with cartilage degradation in osteoarthritis (OA). Because interleukin-1β (IL-1β) has been implicated as a principal instigator of OA, we sought to...

MRT-92 inhibits Hedgehog signaling by blocking overlapping binding sites in the transmembrane domain of the Smoothened receptor.

FASEB J. 29 , 1817-29, (2015)

The Smoothened (Smo) receptor, a member of class F G protein-coupled receptors, is the main transducer of the Hedgehog (Hh) signaling pathway implicated in a wide range of developmental and adult proc...

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