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Cat. No. | Product Name | ||
---|---|---|---|
L4300 | Wnt/Hedgehog/Notch 通路化合物库 | 237 compounds | |
237 个Wnt & Hedgehog & Notch 靶点相关的生物活性小分子化合物的特有集合,用于相关通路的研究及药物的筛选,可用于高通量、高内涵筛选。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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)。 | |||
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。 | |||
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) . | |||
T64351 |
GI-560192
RL-0070933 |
Smo | Stem Cells |
GI-560192 (RL-0070933) 是一种有效的纤毛调节剂。GI-560192 通过 hedgehog 信号通路调节 smoothed (Smo) 向初级纤毛的易位和/或积累。 | |||
T1779 |
SAG
Smoothened Agonist (SAG) HCl,Smoothened Agonist |
Hedgehog/Smoothened; Smo | GPCR/G Protein; Stem Cells |
SAG (Smoothened Agonist) 是一种 Smo 受体激动剂 (EC50=3 nM),具有细胞渗透性和选择性。SAG 可以直接结合 Smo 螺旋束调节 Smo 活性,可以活化 Hedgehog 信号通路。 | |||
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。 | |||
T40465 |
SAG dihydrochloride
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
SAG dihydrochloride 是一种强效的 Smoothened(Smo)受体激动剂(EC 50 =3 nM;K d =59 nM)。SAG dihydrochloride 可激活刺猬信号通路并抵消环丙胺对 Smo 的抑制。 | |||
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。 | |||
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
|
Others | Others |
Glasdegib hydrochloride is a small-molecule inhibitor of the Hedgehog (Hh) signaling pathway with potential antineoplastic activity. | |||
T79055 |
Hedgehog IN-2
|
Others | Others |
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。 | |||
T3363L |
Jervine HCl
Jervine hydrochloride |
Others | Others |
Jervine is a naturally occurring steroidal alkaloid derived from the Veratrum plant species. Over the Hedgehog signaling pathway, Jervine effectively inhibits tumor growth using three human tumor xenograft models. Jervine has the potential to advance to t | |||
T71338 |
Patidegib HCl
|
Others | Others |
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 |
Others | Others |
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 | |||
T71520 |
LEQ-506
|
Others | Others |
LEQ506, also known as NPV-LEQ506, is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Smoothened antagonist LEQ506 selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway, thereby inhibiting tumor cell growth. | |||
T38767 |
MRT-83 hydrochloride
|
Others | Others |
MRT-83 (hydrochloride) is a potent antagonist of the Smoothened (Smo) receptor, effectively inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. With its potential applications in the study of cancer disease, MRT-83 (hydrochloride) demonstrates promising prospects for research purposes. | |||
T40755 |
Glabrescione B
|
Others | Others |
Glabrescione B is a novel compound that specifically binds to Gli1, an important modulator of the Hedgehog (Hh) signaling pathway. By disrupting the Gli1-DNA interaction, Glabrescione B effectively impairs the activity of Gli1. Moreover, Glabrescione B demonstrates potent inhibitory effects on the growth of tumor cells that rely on Hedgehog signaling, as well as on the self-renewal capacity and clonogenicity of tumor-derived stem cells. | |||
T63387 |
SMO-IN-3
|
Others | Others |
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。 | |||
T35538 |
HPI-1 (hydrate)
HPI-1 hydrate |
Others | Others |
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... | |||
T35539 |
IHR-Cy3
IHR-Cy3 |
Others | Others |
Potent fluorescent Smo antagonist (IC50 = 100 nM). Non-fluorescent analog also available. Fan et al (2014) The Hedgehog pathway effector smoothened exhibits signaling competency in the absence of ciliary accumulation. Chem.Biol. 21 1680 PMID:25484239 | |||
T22077 |
Eggmanone
|
Others | Others |
Eggmanone (EGM1) 是一种有效的、选择性的磷酸二酯酶 4(PDE4)拮抗剂,对 PDE4D3 的 IC50为 72 nM。Eggmanone 对 PDE4D3 的选择性大约是其他 PDE 的 40-50 倍。Eggmanone 通过选择性拮抗 PDE4 发挥 Hh 抑制作用,导致蛋白激酶 A 激活和随后的 Hh 阻断。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T1011 |
Itraconazole
伊曲康唑,R51211 |
P450; Hedgehog/Smoothened; Antibiotic; Autophagy; Antifungal | Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Stem Cells |
Itraconazole (R51211) 属于三唑类天然产物,是一种抗真菌剂,具有口服活性。Itraconazole 是一种 Hedgehog 信号通路拮抗剂,一种 oxysterol-binding protein (OSBP) 抑制剂,也是一种细胞色素 P-450 依赖性酶的抑制剂。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-02540 |
GRK2 Protein, Mouse, Recombinant (His & SUMO)
Beta-adrenergic receptor kinase 1,Grk2,G-protein-coupled rec... |
Mouse | E. coli |
Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner. Positively regulates ciliary smoothened (SMO)-dependent Hedgehog (Hh) signaling pathway by facilitating the trafficking of SMO into the cilium and... |