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) | ||
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
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. |
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. |
||
| 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. |
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. |
|
| S8075 |
GANT61GANT61 (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. |
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-4101MK-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 |
JervineJervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. |
||
| S6565 |
JK184JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. |
||
| S9743 |
Ciliobrevin DCiliobrevin 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 |
CyclopamineCyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
(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. |
Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to b-actin and reported under western blot images.
|
|
| S2777 |
PF-5274857PF-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-1SANT-1 directly binds to Smoothened (Smo) receptor with Kd of 1.2 nM and inhibits Smo agonist effects with IC50 of 20 nM. |
(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-833923BMS-833923 (XL139) is an orally bioavailable Smoothened antagonist. Phase 2. |
Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).
|
|
| S6384新 |
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 |
PurmorphaminePurmorphamine (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. |
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) HClSmoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
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. |
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. |
||
| 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. |
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. |
|
| S8075 |
GANT61GANT61 (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. |
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-4101MK-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 |
JervineJervine (11-Ketocyclopamine) is a Hedgehog signaling (IC50=500-700 nM) inhibitor that inhibits the sonic hedgehog (shh) pathway by interacting with smoothened. |
||
| S6565 |
JK184JK184 inhibits Gli in the Hedgehog (Hh) pathway with IC50 of 30 nM in mammalian cells. |
||
| S9743 |
Ciliobrevin DCiliobrevin 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 |
CyclopamineCyclopamine (11-deoxojervine) is a specific Hedgehog (Hh) signaling pathway antagonist of Smoothened (Smo) with IC50 of 46 nM in TM3Hh12 cells. |
2022, 149(1)dev200021 2022, 12(1):359 2021, 10.1038/s41586-021-03703-z |
(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. |
2022, 12(1):7 2021, blood.2020010207 2021, 10.1002/1878-0261.13097 |
Western blot analysis on total cell lysates from renal cancer cell lines treated with NVP-LDE225 at different concentrations. Densitometric measurements were normalised to b-actin and reported under western blot images.
|
| S2777 |
PF-5274857PF-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-1SANT-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 |
(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-833923BMS-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 |
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 |
|---|---|---|---|
| S6384新 |
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. |
2021, e53015 2021, 13(20)3595 |
|
| S3042 |
PurmorphaminePurmorphamine (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. |
2021, 39(3):407-422.e13 2021, 9:679806 2021, 10.1139/cjpp-2020-0588 |
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) HClSmoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells. |
2021, 118(29)e2101783118 2021, e53015 2021, 10e61432 |
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.
|
