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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)
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
E0782 MRT 10 <1 mg/mL 93 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
S9743 Ciliobrevin D <1 mg/mL 20 mg/mL ''<1 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
E0480 MRT-81 <1 mg/mL 100 mg/mL <1 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
S6384 Smoothened Agonist (SAG) <1 mg/mL 98 mg/mL '98 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

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.

S2157

Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

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.

E0782

MRT 10

MRT-10 inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with IC50 of 0.64_x005fμM, showing the capacity to abrogate the constitutive activity of Smo.

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.

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.

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.

S6565

JK184

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.

S9743

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.

S7160

Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.

S1146

Cyclopamine

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 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.

E0480

MRT-81

MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells, exerting potent hedgehog (Hh) signaling pathway inhibiting activity.

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.

S7092

SANT-1

SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

S7138

BMS-833923

BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.

S6384

Smoothened Agonist (SAG)

Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.

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.

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.

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.

S2157

Taladegib (LY2940680)

Taladegib (LY2940680) binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling. Phase 1/2.

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.

E0782

MRT 10

MRT-10 inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with IC50 of 0.64_x005fμM, showing the capacity to abrogate the constitutive activity of Smo.

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.

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.

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.

S6565

JK184

JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells.

S9743

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.

S7160

Glasdegib (PF-04449913)

Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 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
S1146

Cyclopamine

Cyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells.

2022, 38(7):110379

2022, 13(2):136

2022, 2022:9955677

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.

2022, mjab082

2022, 199:115009

2022, 10.1111/cns.13835

E0480

MRT-81

MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells, exerting potent hedgehog (Hh) signaling pathway inhibiting activity.

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.

2022, 12(1):7

2021, ioab111

2020, 41(7):993-1004

S7092

SANT-1

SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM.

2022, 12(1):7

2021, e2103495

2021, 13(2):3199-3208

S7138

BMS-833923

BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2.

2022, 12(1):7

2021, molcanres.MCR-21-0257-A.2021

2020, 41(7):993-1004

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
S6384

Smoothened Agonist (SAG)

Smoothened Agonist (SAG) is potent agonist of Smoothened (Smo). Smoothened Agonist induces firefly luciferase expression in Shh-LIGHT2 cells with an EC50 of 3 nM.

2022, 13(1):2387

2022, 10.1007/s11418-022-01603-8

2021, e53015

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.

2022, 13(1):1439

2022, e2200386

2022, 2022:9955677

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.

2022, 13(1):2733

2022, 13(1):2387

2022, e14990

Tags: Smo activity | smoothened pathway | smoothened pathway | smoothened signaling | Smo cancer | Smo pathway | smoothened signaling pathway | smoothened inhibitor review