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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
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

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.

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) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S4747

Jervine

Jervine 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.

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.

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.

S3042

Purmorphamine

Purmorphamine, 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.

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) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo.

S4747

Jervine

Jervine 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.

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.

2020, 11(1):44

2020, 21;31(3):107521

2020, 7

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.

2020, 18;12(1):17

2020, 30(3):771-782

2020, 41(7):993-1004

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.

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.

2020, 41(7):993-1004

2020, S2213-6711(20)30291-5

2020, 9(9):E1927

S7138

BMS-833923

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

2020, 41(7):993-1004

2019, 2019:3435901

2018, 1148-1154

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, 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.

2020, 10(15):6638-6660

2020, 11(9):755

2020, 159:9-15

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.

2020, 10.1038/s41589-020-0646-2

2020, 202002144

2020, 10.1038/s41401-020-00504-4

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