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信号経路図

研究分野

  • 阻害剤の選択性比較
  • 溶解度
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
S1146 Cyclopamine <1 mg/mL <1 mg/mL 2 mg/mL
S2151 Erismodegib (NVP-LDE225) <1 mg/mL 97 mg/mL 97 mg/mL
S2157 Taladegib (LY2940680) <1 mg/mL 5 mg/mL 2 mg/mL
S3042 Purmorphamine <1 mg/mL 4 mg/mL <1 mg/mL
S8597 LYN-1604 100 mg/mL 50 mg/mL 100 mg/mL
S4747 Jervine <1 mg/mL 5 mg/mL 2 mg/mL
S8249 HPI-4 (Ciliobrevin A) <1 mg/mL 71 mg/mL 1 mg/mL
S2777 PF-5274857 93 mg/mL 93 mg/mL <1 mg/mL
S8075 GANT61 <1 mg/mL <1 mg/mL 12 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
S8200 MK-4101 <1 mg/mL 98 mg/mL 60 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

製品コード 製品説明 文献中の使用例 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.

S1146

Cyclopamine

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

S2151

Erismodegib (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.

S2157

Taladegib (LY2940680)

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

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.

S8597

LYN-1604

S4747

Jervine

Jervine is an inhibitor of Hedgehog signaling (IC50=500-700 nM) that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened.

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.

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.

S8075

GANT61

GANT61 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.

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 is an orally bioavailable Smoothened antagonist. Phase 2.

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.

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.

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