ヘッジホッグ/スムーズンド

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1082	Vismodegib (GDC-0449)	<1 mg/mL	84 mg/mL	<1 mg/mL
S2157	Taladegib (LY2940680)	<1 mg/mL	5 mg/mL	'2 mg/mL
S2476	Itraconazole (R 51211)	<1 mg/mL	7 mg/mL	'''<1 mg/mL
S9743	Ciliobrevin D	<1 mg/mL	20 mg/mL	''<1 mg/mL
S8075	GANT61	<1 mg/mL	<1 mg/mL	''12 mg/mL
S8200	MK-4101	<1 mg/mL	98 mg/mL	60 mg/mL
S8249	HPI-4 (Ciliobrevin A)	<1 mg/mL	71 mg/mL	'1 mg/mL
S4747	Jervine	<1 mg/mL	5 mg/mL	'2 mg/mL
S6565	JK184	<1 mg/mL	70 mg/mL	14 mg/mL
S7160	Glasdegib (PF-04449913)	<1 mg/mL	47 mg/mL	<1 mg/mL
S1146	Cyclopamine	<1 mg/mL	<1 mg/mL	2 mg/mL
S2151	Sonidegib (NVP-LDE225)	<1 mg/mL	97 mg/mL	97 mg/mL
S2777	PF-5274857	93 mg/mL	93 mg/mL	<1 mg/mL
S7092	SANT-1	<1 mg/mL	21 mg/mL	20 mg/mL
S7138	BMS-833923	<1 mg/mL	95 mg/mL	<1 mg/mL
S3042	Purmorphamine	<1 mg/mL	4 mg/mL	'<1 mg/mL
S7779	Smoothened Agonist (SAG) HCl	100 mg/mL	71 mg/mL	40 mg/mL

亜型選択性的な製品

Hedgehog/Smoothened製品

All (17) Hedgehog/Smoothened阻害剤(10) Hedgehog/Smoothened拮抗剤(5) Hedgehog/Smoothened作動薬(2)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1082	Vismodegib (GDC-0449) Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.	Nature, 2021, 10.1038/s41586-021-03703-z Blood, 2021, blood.2020010207 Adv Sci (Weinh), 2021, 8(14):2100626	Relationship between Hh signaling and HCC in HBxTg. A, HCC nodules (circled) on the surface of the liver. B, the number of visible nodules observed on livers ( n = 6 HBxTg per group) after inject ions of vehicle (dark bars) or GDC- 0449 (light bars). Tumor numbers for individual mice are shown above each bar. The average tumor number is shown above each group. C, Western blot analysis for Gli2 in livers from transgenic mice treated with vehicle (-) or GDC- 0449 (+). D, staining for Gli2 and Shh on serial section s of tumors (T) and nontumor (NT) livers from HBxTg treated with vehicle (top) or GDC- 0449 (bottom). Magnification is ?00 for each panel and ?00 for each insert.
S2157	Taladegib (LY2940680) Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.	Carcinogenesis, 2020, 41(7):993-1004 Sci Rep, 2019, 9(1):1897 Front Pharmacol, 2019, 10:89
S2476	Itraconazole (R 51211) Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Sci Rep, 2021, 11(1):17665 Front Microbiol, 2021, 12:649026	Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies.
S9743^新	Ciliobrevin D Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. Ciliobrevin D perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.
S8075	GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.	Blood, 2021, blood.2020010207 J Bone Miner Res, 2021, 10.1002/jbmr.4265 Cell Death Dis, 2021, 12(5):495	Apoptosis evaluation of UACC62R, SK-MEL-28 R and R3 cells treated with Gant61 (10 μM) for 48 h by flow cytometry detection of Annexin V staining.
S8200	MK-4101 MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
S8249	HPI-4 (Ciliobrevin A) HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.	FASEB J, 2020, 10.1096/fj.201901852RR Front Pharmacol, 2019, 10:290 PLoS One, 2019, 14(5):e0216642
S4747	Jervine Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.	Neurochem Int, 2021, 146:105042
S6565	JK184 JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.	Cell Res, 2020, 10.1038/s41422-020-00426-0
S7160	Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.	Genome Med, 2020, 18;12(1):17
S1146	Cyclopamine Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.	Nature, 2021, 10.1038/s41586-021-03703-z Neuron, 2021, S0896-6273(21)00506-7 Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118	(A)[3H]thymidine incorporation assay of B16F10 melanoma cells treated with DMSO or cyclopamine after incubation with SA-CM from WT and Cav1KO dermal fibroblasts. Representative phase-contrast images of B16F10 cells treated with SA-CM from WT and Cav1KO fibroblasts with cyclopamine are shown on the right. Similar experiments (B) were done with A-375 cells incubated with SA-CM from hTBJ1-shCtrl and hTBJ1-shCAV1 cells.
S2151	Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.	Blood, 2021, blood.2020010207 Sci Rep, 2021, 11(1):17665 Genome Med, 2020, 18;12(1):17	NVP-LDE225, everolimus, sunitinib, and their combination interfere with actin and with intracellular organisation of focal adhesion points. Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 ( 2.5 uM ), everolimus (1 uM ), sunitinib (1 uM ), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
S2777	PF-5274857 PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.	Biol Reprod, 2021, ioab111 Carcinogenesis, 2020, 41(7):993-1004
S7092	SANT-1 SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.	ACS Appl Mater Interfaces, 2021, 13(2):3199-3208 J Ethnopharmacol, 2021, S0378-8741(21)00863-1 Carcinogenesis, 2020, 41(7):993-1004	(D) Percentage cell death of OCI-AML3 cells was measured using the CellTiter-Glo® viability assay following 24 hours treatment with either sequential treatment of 1 μM Vorinostat with low (0.1 μM) or high dose (2.5 μM) SANT-1, or single agents. Data represents a biological replicate of 3, with data presented relative to the DMSO control (0% cell death). (E) Protein expression of SHH was measured following 24 hours treated with the four treatment strategies in OCI-AML3 cells. Equal loading was confirmed with β-Actin
S7138	BMS-833923 BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.	Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021 Carcinogenesis, 2020, 41(7):993-1004 Stem Cells Int, 2019, 2019:3435901	Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).
S3042	Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.	Cancer Cell, 2021, 39(3):407-422.e13 Can J Physiol Pharmacol, 2021, 10.1139/cjpp-2020-0588 Theranostics, 2020, 10(15):6638-6660	a-d) LoVo cells were separately or simultaneously treated with 1 μM purmorphamine and 1 μM thiostrepton for the indicated time. a The Gli1, FoxM1, and CCNB1 protein expression levels were examined by immunoblotting after drug treatment for 48 h. b Cell viability was detected after 6 days using an MTT assay. c LoVo cells treated with indicated drugs were cultured for 2 weeks, and outgrowth colonies were stained with crystal violet. d The matched colony count of (c). Error bars represent the mean and S.D. of three independent experiments. **, p < 0.01.
S7779	Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.	Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118 Elife, 2021, 10e61432 Front Cell Dev Biol, 2021, 9:621442	Activating Shh signaling by SAG injection in naïve mice significantly increased BDNF expression, and pretreatment with cyclopamine effectively prevented the upregulation of BDNF induced by SAG (E). Tissues were collected at 2 hours after SAG injection. Six mice were included in each group.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1082	Vismodegib (GDC-0449) Vismodegib (GDC-0449) is a potent, novel and specific hedgehog inhibitor with IC50 of 3 nM and also inhibits P-gp with IC50 of 3.0 μM in a cell-free assay.	Nature, 2021, 10.1038/s41586-021-03703-z Blood, 2021, blood.2020010207 Adv Sci (Weinh), 2021, 8(14):2100626	Relationship between Hh signaling and HCC in HBxTg. A, HCC nodules (circled) on the surface of the liver. B, the number of visible nodules observed on livers ( n = 6 HBxTg per group) after inject ions of vehicle (dark bars) or GDC- 0449 (light bars). Tumor numbers for individual mice are shown above each bar. The average tumor number is shown above each group. C, Western blot analysis for Gli2 in livers from transgenic mice treated with vehicle (-) or GDC- 0449 (+). D, staining for Gli2 and Shh on serial section s of tumors (T) and nontumor (NT) livers from HBxTg treated with vehicle (top) or GDC- 0449 (bottom). Magnification is ?00 for each panel and ?00 for each insert.
S2157	Taladegib (LY2940680) Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.	Carcinogenesis, 2020, 41(7):993-1004 Sci Rep, 2019, 9(1):1897 Front Pharmacol, 2019, 10:89
S2476	Itraconazole (R 51211) Itraconazole (R 51211) is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent. Itraconazole is a potent antagonist of the Hedgehog (Hh) signaling pathway. Itraconazole suppresses the growth of glioblastoma through induction of autophagy.	Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4 Sci Rep, 2021, 11(1):17665 Front Microbiol, 2021, 12:649026	Resistance to itraconazole in MA cells. The parental SUM149-Luc cell line and MA1 cells were treated in parallel with 1 mM itraconazole for 9 days (which killed most of the cells in the parental cell line) and were allowed to recover and grow in a drug-free medium for 5 days before being stained. Since itraconazole was ineffective in killing MA1 cells, the cells grew into a continuous monolayer rather than colonies.
S9743^新	Ciliobrevin D Ciliobrevin D (compound 5) is a cell-permeable, reversible and specific antagonist of AAA+ (ATPases associated with diverse cellular activities) ATPase motor cytoplasmic dynein. Ciliobrevin D perturbs primary cilia formation and blocks Hedgehog (Hh) signaling.
S8075	GANT61 GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.	Blood, 2021, blood.2020010207 J Bone Miner Res, 2021, 10.1002/jbmr.4265 Cell Death Dis, 2021, 12(5):495	Apoptosis evaluation of UACC62R, SK-MEL-28 R and R3 cells treated with Gant61 (10 μM) for 48 h by flow cytometry detection of Annexin V staining.
S8200	MK-4101 MK-4101, a potent inhibitor of the Hedgehog pathway, shows anti-tumor activity through the inhibition of proliferation and induction of extensive apoptosis in tumor cells.
S8249	HPI-4 (Ciliobrevin A) HPI-4 (Ciliobrevin A, Hedgehog Pathway Inhibitor 4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.	FASEB J, 2020, 10.1096/fj.201901852RR Front Pharmacol, 2019, 10:290 PLoS One, 2019, 14(5):e0216642
S4747	Jervine Jervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.	Neurochem Int, 2021, 146:105042
S6565	JK184 JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.	Cell Res, 2020, 10.1038/s41422-020-00426-0
S7160	Glasdegib (PF-04449913) Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.	Genome Med, 2020, 18;12(1):17

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1146	Cyclopamine Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.	Nature, 2021, 10.1038/s41586-021-03703-z Neuron, 2021, S0896-6273(21)00506-7 Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118	(A)[3H]thymidine incorporation assay of B16F10 melanoma cells treated with DMSO or cyclopamine after incubation with SA-CM from WT and Cav1KO dermal fibroblasts. Representative phase-contrast images of B16F10 cells treated with SA-CM from WT and Cav1KO fibroblasts with cyclopamine are shown on the right. Similar experiments (B) were done with A-375 cells incubated with SA-CM from hTBJ1-shCtrl and hTBJ1-shCAV1 cells.
S2151	Sonidegib (NVP-LDE225) Sonidegib (Erismodegib, NVP-LDE225) is a Smoothened (Smo) antagonist, inhibiting Hedgehog (Hh) signaling with IC50 of 1.3 nM (mouse) and 2.5 nM (human) in cell-free assays, respectively. Phase 3.	Blood, 2021, blood.2020010207 Sci Rep, 2021, 11(1):17665 Genome Med, 2020, 18;12(1):17	NVP-LDE225, everolimus, sunitinib, and their combination interfere with actin and with intracellular organisation of focal adhesion points. Cytoskeleton organisation of 786-O SuR treated with NVP-LDE225 ( 2.5 uM ), everolimus (1 uM ), sunitinib (1 uM ), and their combination for 24 h was analysed by confocal microscopy. Actin-based structures were revealed by rhodaminated phalloidin staining (red fluorescence). Localisation of focal adhesion points was obtained by immunofluorescent staining of p-paxillin (green fluorescence). Merged row images show overlapping of p-paxillin and actin signals. Moreover, all captures were shown in transmitted light. Scale bars, 10 um.
S2777	PF-5274857 PF-5274857 is a potent and selective Smoothened (Smo) antagonist, inhibits Hedgehog (Hh) signaling with IC50 and Ki of 5.8 nM and 4.6 nM, respectively, and can penetrate the blood–brain barrier.	Biol Reprod, 2021, ioab111 Carcinogenesis, 2020, 41(7):993-1004
S7092	SANT-1 SANT-1 directly binds to Smoothened (Smo) receptor with K_d of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.	ACS Appl Mater Interfaces, 2021, 13(2):3199-3208 J Ethnopharmacol, 2021, S0378-8741(21)00863-1 Carcinogenesis, 2020, 41(7):993-1004	(D) Percentage cell death of OCI-AML3 cells was measured using the CellTiter-Glo® viability assay following 24 hours treatment with either sequential treatment of 1 μM Vorinostat with low (0.1 μM) or high dose (2.5 μM) SANT-1, or single agents. Data represents a biological replicate of 3, with data presented relative to the DMSO control (0% cell death). (E) Protein expression of SHH was measured following 24 hours treated with the four treatment strategies in OCI-AML3 cells. Equal loading was confirmed with β-Actin
S7138	BMS-833923 BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.	Mol Cancer Res, 2021, molcanres.MCR-21-0257-A.2021 Carcinogenesis, 2020, 41(7):993-1004 Stem Cells Int, 2019, 2019:3435901	Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S3042	Purmorphamine Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.	Cancer Cell, 2021, 39(3):407-422.e13 Can J Physiol Pharmacol, 2021, 10.1139/cjpp-2020-0588 Theranostics, 2020, 10(15):6638-6660	a-d) LoVo cells were separately or simultaneously treated with 1 μM purmorphamine and 1 μM thiostrepton for the indicated time. a The Gli1, FoxM1, and CCNB1 protein expression levels were examined by immunoblotting after drug treatment for 48 h. b Cell viability was detected after 6 days using an MTT assay. c LoVo cells treated with indicated drugs were cultured for 2 weeks, and outgrowth colonies were stained with crystal violet. d The matched colony count of (c). Error bars represent the mean and S.D. of three independent experiments. **, p < 0.01.
S7779	Smoothened Agonist (SAG) HCl Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.	Proc Natl Acad Sci U S A, 2021, 118(29)e2101783118 Elife, 2021, 10e61432 Front Cell Dev Biol, 2021, 9:621442	Activating Shh signaling by SAG injection in naïve mice significantly increased BDNF expression, and pretreatment with cyclopamine effectively prevented the upregulation of BDNF induced by SAG (E). Tissues were collected at 2 hours after SAG injection. Six mice were included in each group.

製品コード

製品説明

文献中Selleckの製品使用例

お客様のフィードバック

S3042

Purmorphamine

Purmorphamine (Shh Signaling Antagonist VI), which directly binds and activates Smoothened, blocks BODIPY-cyclopamine binding to Smo with IC50 of ~ 1.5 μM in HEK293T cell and also is an inducer of osteoblast differentiation with EC50 of 1 μM. Purmorphamine can reduce both basal and induced autophagy.

Cancer Cell, 2021, 39(3):407-422.e13

Can J Physiol Pharmacol, 2021, 10.1139/cjpp-2020-0588

Theranostics, 2020, 10(15):6638-6660