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Search Results for " smoothened "

52

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T4211	SAG hydrochloride (912545-86-9(free base)) Smoothened Agonist HCl	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	SAG hydrochloride (912545-86-9(free base)) (Smoothened Agonist HCl) 可作为 SMO 激动剂。
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。
T22814	GSA-10	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	GSA-10是新型的喹啉甲酰胺衍生物，有效激动平滑受体剂，EC50为 1.2 μM。它作用于Smo，促进多能间充质干细胞分化为成骨细胞。它介导 Hedgehog 信号传导，这可能对癌症疾病的再生医学具有研究意义。
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。
T9531	MRT-14	Smo	Stem Cells
	MRT-14 是有效的 Smo 拮抗剂。Smo 是参与 Hedgehog 形态发生素信号转导的主要成分。MRT-14 在研究与异常 Hh 信号传导相关的多种癌症方面有价值。
T12109	MRT-83	Smo	Stem Cells
	MRT-83 是一种 Smo 拮抗剂，其IC50值在纳摩尔级别。它能够抑制 Hedgehog 信号通路。
T6514	Glasdegib PF-04449913	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	Glasdegib (PF-04449913) 是一种口服具有活力的 smoothened 抑制剂，能够结合到人 SMO(181-787氨基酸位点)，IC50=4 nM。
T2450	SANT-1 SANT 1	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	SANT-1 是Smo 拮抗剂，能够抑制Hedgehog 通路，在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中，得到的IC50值分别为 20 nM 和 30 nM。
T14188	ALLO-2	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	ALLO-2 是一种 Smo 耐药突变体的拮抗剂。在TM3-Gli-Luc 细胞中，它可抑制Smo 激动剂Hh-Ag1.5诱导的荧光素酶表达，其IC50=6 nM。
T24159	IHR-1 IHR 1	Smo	Stem Cells
	IHR-1 是一种Smo 拮抗剂，不能透过细胞膜。
T2666	Taladegib LY2940680	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	Taladegib (LY2940680) 是smoothened 受体拮抗剂。
T9532	MRT-81	Others	Others
	MRT-81 是一种人和啮齿动物 smoothened 受体的有效拮抗剂，能够抑制 hedgehog 的活性，在 Shh-light2 细胞中的IC50值为 41 nM。它可用于研究癌症。
T1810	Purmorphamine Shh Signaling Antagonist VI	Hedgehog/Smoothened; Smo; Autophagy	Autophagy; GPCR/G Protein; Stem Cells
	Purmorphamine (Shh Signaling Antagonist VI) 是平滑受体激动剂，EC50为 1 μM。它阻止 BODIPY-cyclopamine 与 Smo 结合。它也是成骨细胞分化的诱导剂。
T23027	MRT-10	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	MRT 10 是一种七跨膜平滑受体 (Smo) 拮抗剂，通过多种 Hedgehog (Hh) 测定，其IC50=0.65 μM。它与Smo 受体结合的位点是 Bodipycyclopamine。它可用于研究癌症。
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。
T2299	BMS-833923 XL-139	Apoptosis; Hedgehog/Smoothened; Smo	Apoptosis; GPCR/G Protein; Stem Cells
	BMS-833923 (XL-139) 是一种口服生物可利用的 Smoothened 拮抗剂，以剂量依赖性方式抑制 BODIPY cyclopamine 与 SMO 的结合，IC50为21 nM。
T11838	LEQ506 NVP-LEQ506	Smo	Stem Cells
	LEQ506 是一种 Smo 抑制剂，对 hSmo 和 mSmo 的 IC50 分别为 2 nM 和 4 nM。
T0107	Halcinonide Halcimat,Halciderm,哈西奈德,Halcinonida,氯氟舒松,SQ-18566	Glucocorticoid Receptor; Smo	Endocrinology/Hormones; Stem Cells
	Halcinonide (Halciderm) 是一种糖皮质激素，可用于局部皮肤感染的研究。
T1926	Sonidegib Erismodegib,NVP-LDE225,LDE225	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	Sonidegib (Erismodegib) 是一种Smo 的选择性拮抗剂，能够抑制鼠 Smo (IC50:1.3 nM)和人 Smo (IC50:2.5 nM)。
T2250	DY131 DY 131,GSK 9089,DY-131	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Smo	Endocrinology/Hormones; Stem Cells
	DY131 (DY-131) 是选择性的 ERRγ 和 ERRβ 激动剂，对 ERRα，ERα 和 ERβ 无效。它对Smo 的信号传导具有抑制作用。
T15727	Sonidegib diphosphate NVP-LDE 225 diphosphate,Erismodegib diphosphate,LDE225 diphosphate	Smo	Stem Cells
	Sonidegib diphosphate (LDE225 diphosphate) 是 Smo 的选择性拮抗剂，能够抑制鼠 Smo (IC50:1.3 nM)和人 Smo (IC50:2.5 nM)。
T23370	SMANT hydrochloride N-(4-Bromophenyl)-3,5-dimethyl-1-piperidinepropanamide hydrochloride,hydrochloride,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide;hydrochloride,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide,SMANT HCl,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide hydrochloride	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	SMANT hydrochloride (N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide hydrochloride) 是一种 Smoothened 积聚的拮抗剂。
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)。
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。
T63429	SMO-IN-2	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	SMO-IN-2 是一种有效的 smoothened (SMO) 抑制剂，对 hedgehog (Hh) 信号传导有抑制作用。SMO-IN-2 对人髓母细胞瘤细胞系显示出抗增殖活性和抗癌活性。SMO-IN-2 可用于研究癌症。
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。
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。
T24754	Hh-Ag1.5 SAG-1.5,SAG1.5,SAG 1.5	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	Hh-Ag1.5 (SAG-1.5) 是一种高效的 Hedgehog (Hh) 激动剂(EC50： 1 nM)和Smoothened (Smo)受体激动剂，对Smo的 EC50 为 1 nM、 Ki值在 0.5 和 2.3 nM 之间。Hh-Ag1.5 介导的重编程打破了非损伤肝脏干细胞的静止状态，从而挽救了肝衰竭。Hh-Ag1.5 诱导 hiPSCs 分化为皮肤前体细胞、脊髓运动神经元和脊髓感觉神经元。
T22958	M 25	Others	Others
	Smoothened (Smo) receptor antagonist
T71299	M-25
	M-25 is a Smoothened antagonist and inhibitor of the Hedgehog pathway.
T71520	LEQ-506
	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.
T70178	Sonidegib metabolite M25
	Sonidegib metabolite M25 is a smoothened (SMO) antagonist.
T61895	AZD7254
	AZD7254 是有口服有效的Smoothened (SMO)抑制剂， sonic Hh protein (shh) 的EC50为 1.0 nM。
T26723	AZD8542 AZD-8542,AZD 8542
	AZD8542 is an antagonist of Smoothened (SMO) with potential as an oncology therapeutic.
T23307	SANT 2 SANT-2	Others	Others
	SANT-2 is an inhibitor of Sonic hedgehog signaling and also antagonizes smoothened receptor activity (KD = 12 nM).
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.
T24400	LEQ-506 HCl (1204975-42-7 free base) LEQ-506,LEQ-506 dihychloride,NPVLEQ 506,LEQ506,LEQ-506 HCl,LEQ 506
	LEQ506 is an orally bioavailable small-molecule Smoothened antagonist. It also has a potential antineoplastic activity.
T61897	SMO-IN-1
	SMO-IN-1 (Compound 15) 是口服有效的Smoothened (SMO)抑制剂， sonic Hh protein (shh) 的EC50值为 89 nM。
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。
T25918	Palmitoyl-L-aspartic acid L-N-Palmitoylaspartic acid
	Palmitoyl-L-aspartic acid is a natural N-acylaspartate that suppresses Hedgehog signaling after stimulation with Smoothened agonist or non-sterol-modified Sonic Hedgehog. It does not alter the activity of cannabinoid receptors or fatty acid amide hydrolas
T38767	MRT-83 hydrochloride
	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.
T62772	TPB15
	TPB15 是一种口服具有活力的 Hh(Hedgehog) 信号抑制剂。TPB15 可以明显阻滞 MDA-MB-468 细胞周期，并诱导其凋亡。TPB15 阻断 Smo(Smoothened) 转位到纤毛中，减少 Smo 蛋白和 mRNA 表达。TPB15 对下游调控因子胶质瘤相关癌基因1 (Gli1) 的表达表现出抑制作用。TPB15 具有较好的抗肿瘤作用，且毒性较低。
T70693	MRT-92 HCl salt
	MRT-92 is a potent and selective Smoothened (Smo) receptor inhibitor. MRT-92 displays subnanomolar antagonist activity against Smo in various Hh cell-based assays. MRT-92 inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation through pharmacologic (half maximal inhibitory concentration [IC50] = 0.4 nM) or genetic manipulation. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain.
T35539	IHR-Cy3 IHR-Cy3
	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
T35537	Hedgehog Antagonist VIII
	Hedgehog (Hh) proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of Smoothened. In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the Gli family. Overactivation of this pathway contributes to certain cancers, including glioblastoma, for which the Gli proteins are named. Hh antagonist VIII is a cell-permeable quinazolinyl-urea compound that has been shown to inhibit Gli transcription activity ...
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...
T36910	PF 04449913 maleate
	Potent Smo antagonist (IC50 = 5 nM). Attenuates the leukemia-initiation potential of AML cells in a serial transplantation mouse model. Also eliminates self-propagation capacity of AML cells. Munchhof et al (2011) Discovery of PF-04449913, a potent and orally bioavailable inhibitor of smoothened. ACS Med.Chem.Lett. 3 106 PMID:24900436 \|Fukushima et al (2016) Small-molecule Hedgehog inhibitor attenuates the leukemia-initiation potential of acute myeloid leukemia cells. Cancer Sci. 107 1422 PMID:2...
T35538	HPI-1 (hydrate) HPI-1 hydrate
	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...
T35558	KAAD-Cyclopamine
	Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated onco...

化合物

Cat.No: T1779

Synonym: Smoothened Agonist (SAG) HCl,Smoothened Agonist

Target: Hedgehog/Smoothened, Smo

SAG hydrochloride (912545-86-9(free base))

Cat.No: T4211

Synonym: Smoothened Agonist HCl

Target: Hedgehog/Smoothened

Cat.No: T3460

Target: Hedgehog/Smoothened, Smo

Cat.No: T22814

Target: Hedgehog/Smoothened

Cat.No: T6891

Target: Apoptosis, Hedgehog/Smoothened, Smo

Cat.No: T9531

Target: Smo

Cat.No: T12109

Target: Smo

Cat.No: T6514

Synonym: PF-04449913

Target: Hedgehog/Smoothened, Smo

Cat.No: T2450

Synonym: SANT 1

Target: Hedgehog/Smoothened, Smo

Cat.No: T14188

Target: Hedgehog/Smoothened, Smo

Cat.No: T24159

Synonym: IHR 1

Target: Smo

Cat.No: T2666

Synonym: LY2940680

Target: Hedgehog/Smoothened, Smo

Cat.No: T9532

Target: Others

Cat.No: T1810

Synonym: Shh Signaling Antagonist VI

Target: Hedgehog/Smoothened, Smo, Autophagy

Cat.No: T23027

Target: Hedgehog/Smoothened

Cat.No: T5465

Synonym: PF-5274857 freebase

Target: Smo

Cat.No: T2299

Synonym: XL-139

Target: Apoptosis, Hedgehog/Smoothened, Smo

Cat.No: T11838

Synonym: NVP-LEQ506

Target: Smo

Cat.No: T0107

Synonym: Halcimat,Halciderm,哈西奈德,Halcinonida,氯氟舒松,SQ-18566

Target: Glucocorticoid Receptor, Smo

Cat.No: T1926

Synonym: Erismodegib,NVP-LDE225,LDE225

Target: Hedgehog/Smoothened, Smo

Cat.No: T2250

Synonym: DY 131,GSK 9089,DY-131

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Smo

Sonidegib diphosphate

Cat.No: T15727

Synonym: NVP-LDE 225 diphosphate,Erismodegib diphosphate,LDE225 diphosphate

Target: Smo

SMANT hydrochloride

Cat.No: T23370

Synonym: N-(4-Bromophenyl)-3,5-dimethyl-1-piperidinepropanamide hydrochloride,hydrochloride,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide;hydrochloride,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide,SMANT HCl,N-(4-bromophenyl)-3-(3,5-dimethylpiperidin-1-yl)propanamide hydrochloride

Target: Hedgehog/Smoothened

Cat.No: T15019

Target: Hedgehog/Smoothened

SAG dihydrochloride

Cat.No: T40465

Target: Hedgehog/Smoothened

Cat.No: T63429

Target: Hedgehog/Smoothened

CUR61414 hydrochloride

Cat.No: T15019L

Synonym: CUR61414 hydrochloride (334998-36-6 Free base)

Target: Hedgehog/Smoothened

Cat.No: T64351

Synonym: RL-0070933

Target: Smo

Cat.No: T24754

Synonym: SAG-1.5,SAG1.5,SAG 1.5

Target: Hedgehog/Smoothened

Cat.No: T22958

Target: Others

Cat.No: T71299

Cat.No: T71520

Sonidegib metabolite M25

Cat.No: T70178

Cat.No: T61895

Cat.No: T26723

Synonym: AZD-8542,AZD 8542

Cat.No: T23307

Synonym: SANT-2

Target: Others

Cat.No: T16843

Synonym: IPI-926,Patidegib

Target: Others

LEQ-506 HCl (1204975-42-7 free base)

Cat.No: T24400

Synonym: LEQ-506,LEQ-506 dihychloride,NPVLEQ 506,LEQ506,LEQ-506 HCl,LEQ 506

Cat.No: T61897

Cat.No: T63387

Palmitoyl-L-aspartic acid

Cat.No: T25918

Synonym: L-N-Palmitoylaspartic acid

MRT-83 hydrochloride

Cat.No: T38767

Cat.No: T62772

MRT-92 HCl salt

Cat.No: T70693

Cat.No: T35539

Synonym: IHR-Cy3

Hedgehog Antagonist VIII

Cat.No: T35537

Cat.No: T70195

PF 04449913 maleate

Cat.No: T36910

HPI-1 (hydrate)

Cat.No: T35538

Synonym: HPI-1 hydrate

KAAD-Cyclopamine

Cat.No: T35558

Cat. No.	Product Name	Target	Signaling Pathways
T2825	Cyclopamine 环巴胺,11-Deoxojervine	Hedgehog/Smoothened; Endogenous Metabolite; Smo	GPCR/G Protein; Metabolism; Stem Cells
	Cyclopamine (11-Deoxojervine) 是Hedgehog 通路的拮抗剂，细胞实验中IC50=46 nM。它还是选择性Smo 抑制剂。
T3363	Jervine 蒜黎芦碱,Iervin,11-Ketocyclopamine,Jerwiny	Hedgehog/Smoothened; Smo	GPCR/G Protein; Stem Cells
	Jervine (Jerwiny) 是一种有效的刺猬 (Hh) 抑制剂(IC50:500-700 nM)。它是一种天然致畸性甾体生物碱，来自于 Veratrumalbum 的根茎，具有抗炎和抗氧化作用。
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。
T10085	20(S)-Hydroxycholesterol 20α-Hydroxycholesterol	Smo	Stem Cells
	20(S)-Hydroxycholesterol (20α-Hydroxycholesterol) 是平滑 (smo) 癌蛋白的变构激活剂。

天然产物

Cat.No: T2825

Synonym: 环巴胺,11-Deoxojervine

Target: Hedgehog/Smoothened, Endogenous Metabolite, Smo

Cat.No: T3363

Synonym: 蒜黎芦碱,Iervin,11-Ketocyclopamine,Jerwiny

Target: Hedgehog/Smoothened, Smo

Saikosaponin B1

Cat.No: T3912

Synonym: 柴胡皂苷B1,柴胡皂苷 B1

Target: Others

20(S)-Hydroxycholesterol

Cat.No: T10085

Synonym: 20α-Hydroxycholesterol

Target: Smo

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