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Cat. No. | Product Name | Target | Signaling Pathways |
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T3156 |
Ciliobrevin A
Hedgehog Pathway Inhibitor 4,HPI-4 |
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
Ciliobrevin A (HPI-4) 是Hedgehog(Hh) 信号通路抑制剂,平均抑制浓度 (IC50) 值小于 10 μM。 | |||
T20723 |
LGE-899
Sonidegib metabolite M48,LGE 899 |
Drug Metabolite | Metabolism |
LGE-899 (Sonidegib metabolite M48) 是 Sonidegib 的主要代谢物,是一种刺猬通路抑制剂。 LGE-899 (60 h) 的 Tmax 比 Sonidegib 长得多。 | |||
T3588 |
JK184
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
JK184 是 Hedgehog 抑制剂,在哺乳动物细胞中的IC50值为 30 nM。 | |||
T3460 |
HhAntag
|
Hedgehog/Smoothened; Smo | GPCR/G Protein; Stem Cells |
HhAntag 是高效的、特异性的、具有口服活性的 Hh 通路的SMO 拮抗剂。 | |||
T22089 |
HPI 1
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
HPI 1 是一种刺猬 (Hh) 信号抑制剂。在 Shh-LIGHT2 细胞中抑制 Sonic Hedgehog (Shh)-、SAG- 和 Gli 诱导的 Hh 通路激活(Shh-、SAG-、Gli2- 和 Gli1 诱导的激活的 IC50 值为 1.5、1.5、4 和 6 μM) . | |||
T15019L |
CUR61414 hydrochloride
CUR61414 hydrochloride (334998-36-6 Free base) |
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
CUR61414 hydrochloride 是属于氨基脯氨酸类化合物的小分子。CUR61414 hydrochloride 是一种细胞渗透性的 Hedgehog 信号通路抑制剂(IC50= 100-200 nM),可选择性结合 Smoothened (Smo, Ki= 44 nM)。CUR61414 hydrochloride 可以诱导癌细胞凋亡 (apoptosis) 而不影响非癌症细胞。 | |||
T6891 |
MK-4101
|
Apoptosis; Hedgehog/Smoothened; Smo | Apoptosis; GPCR/G Protein; Stem Cells |
MK-4101 是一种 SMO 拮抗剂 ,对 293 细胞的 IC50为 1.1 µM。它也是一种 hedgehog 信号通路的有效抑制剂 ,对小鼠细胞和KYSE180 食管癌细胞的IC50分别为 1.5 µM 和 1 µM。它能抗肿瘤,抑制肿瘤细胞增殖并诱导细胞凋亡。 | |||
T2590 |
Vismodegib
Erivedge,GDC-0449,RG 3616,维莫德吉 |
Hedgehog/Smoothened; ABC; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Stem Cells |
Vismodegib (GDC-0449) 是一种刺猬抑制剂,IC50值为 3 nM。它还可抑制 P-gp 和ABCG2的活性,IC50值分别为 3.0 μM 和 1.4 μM。 | |||
T12797 |
RU-SKI 43
RUSKI 43 |
Hedgehog/Smoothened; Acyltransferase | GPCR/G Protein; Metabolism; Stem Cells |
RU-SKI 43 是一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂,IC50 为 850 nM。RU-SKI 43 具有抗癌活性,是治疗肺腺癌的潜在化合物。RU-SKI 43 通过独立于平滑化的非规范信号传导降低 Gli-1 激活,并抑制 Akt 和 mTOR 通路活性。 | |||
T5465 |
PF-5274857
PF-5274857 freebase |
Smo | Stem Cells |
PF-5274857 (PF-5274857 free base) freebase 是有效的、具有口服活性的、选择性的、可透过血脑屏障的 Smo 拮抗剂,其 IC50=5.8 nM,Ki=4.6 nM。它有用于包括激活的 Hh 途径驱动的脑肿瘤和脑转移在内的多种肿瘤的研究潜力。 | |||
T71299 |
M-25
|
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M-25 is a Smoothened antagonist and inhibitor of the Hedgehog pathway. | |||
T75148 | Hedgehog IN-3 | ||
HedgehogIN-3 (化合物 3) 是一种hedgehog 通路抑制剂 (IC50= 0.01 µM)。HedgehogIN-3 可用于癌症的研究。 | |||
T16843 |
Saridegib
IPI-926,Patidegib |
Others | Others |
Saridegib is an effective and specific inhibitor of Smoothened and a key signaling transmembrane protein in the Hedgehog pathway. | |||
T71455 | Glasdegib hydrochloride | ||
Glasdegib hydrochloride is a small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. | |||
T79055 |
Hedgehog IN-2
|
||
HedgehogIN-2 (Compound 20)为一Hedgehog信号通路抑制剂,其在C3H10T1/2细胞中表现出低于0.003 μM的IC50值。 | |||
T15019 |
CUR61414
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
CUR61414 是 Hedgehog 信号通路的细胞渗透性抑制剂 (IC50 = 100-200 nM),并选择性地结合 smoothened (Ki = 44 nM)。 | |||
T71338 | Patidegib HCl | ||
Patidegip, laos known as Saridegib and IPI-926, is an orally bioavailable, cyclopamine-derived (for structure comparison see Fig 1) inhibitor of the Hedgehog (Hh) pathway with potential antineoplastic activity. Specifically, Hedgehog pathway inhibitor IPI-926 binds to and inhibits the cell membrane-spanning G-protein coupled receptor SMO, which may result in the suppression of Hh pathway signaling and a decrease in tumor cell proliferation and survival. SMO is activated upon binding of Hh ligan... | |||
T28388 |
PF-5274857 mseylate (1373615-35-0 free base)
PF5274857 HCl,PF 5274857,PF-5274857,PF-5274857 mesylate,PF-5274857 mseylate |
||
PF-5274857 is a potent, orally active and selective inhibitor of hedgehog (Hh) signaling pathway (IC50 = 5.8 nM, Ki = 4.6 nM) . PF-5274857 effectively penetrates the blood-brain barrier and inhibits Smo activity in the brain of primary medulloblastoma mic | |||
T79907 |
HPP-9
|
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HPP-9为一种蛋白降解靶向嵌合体(PROTACs),基于Hedgehog通路抑制剂(HPI-1)开发,pIC50值为6.71,能够降解BET溴结构域,并表现出抗肿瘤活性[1]。 | |||
T70195 | NL-103 | ||
NL-103 is a novel dual-targeted inhibitor of histone deacetylases and hedgehog pathway, effectively overcomes vismodegib resistance conferred by Smo mutations. NL-103 comprises structural elements of Hh pathway inhibitor vismodegib, and histone deacetylase (HDAC) inhibitor vorinostat. NL-103 simultaneously and significantly inhibited both HDACs and Hh pathway. Importantly, NL-103 effectively overcame vismodegib resistance induced by Smoothened point mutations. Moreover, NL-103 significantly dow... | |||
T63387 |
SMO-IN-3
|
||
SMO-IN-3 是 smoothened (SMO) 对有效抑制剂,能够作用于 hedgehog (Hh) 信号通路 (IC50: 34.09 nM)。SMO-IN-3 能够抑制人髓母细胞瘤细胞系 Daoy 的增殖,表现出抗癌作用。 | |||
T72726 |
3-epi-Vitamin D3
Epicholecalciferol |
||
3-epi-Vitamin D3 (Epicholecalciferol) 是维生素 D3 类似物,是一种Hedgehogpathway 抑制剂,在U87MG 细胞中测定的IC50为 39.2 μM。 | |||
T35538 |
HPI-1 (hydrate)
HPI-1 hydrate |
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HPI-1 (hydrate) is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Sonic Hh (IC50= 1.5 μM) without significantly affecting Wnt signaling (IC50≥ 30 μM).1HPI-1 suppresses Hh activation induced by loss of Suppressor of Fused or by Gli overexpression, suggesting action at posttranslational modification of Gli protein or at the interaction of Gli with a co-factor.1HPI-1 (hydrate) also inhibits signaling through the oncogenic Smoothened (Smo) mutant SmoM2 in neuron precursors, prev... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T3912 |
Saikosaponin B1
柴胡皂苷B1,柴胡皂苷 B1 |
Others | Others |
Saikosaponin B1 是柴胡的生物活性成分,具有抗癌作用。它能够靶向SMO 抑制 Hedgehog 通路,显著抑制髓母细胞瘤模型中的肿瘤生长。 |