Hedgehog/Smoothened
信号通路图
研究领域
抑制剂选择性比较
Hedgehog/Smoothened产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1082 |
Vismodegib (GDC-0449)Vismodegib (GDC-0449)是一种新型有效的，特异性hedgehog抑制剂，无细胞试验中IC50为3 nM，也会抑制P-gp，IC50为3.0μM。 |
SMOΔC captured on cholesterol beads in the presence of increasing concentrations of free vismodegib or 20(S)-OHC (h). Results from one of two independent pull-down experiments are shown. |
|
| S2157 |
Taladegib (LY2940680)Taladegib (LY2940680)与Smoothened(Smo)受体结合，有效抑制Hedgehog(Hh)信号通路。Phase 1/2。 |
||
| S8075 |
GANT61GANT61是一种GLI1及GLI2诱导的转录抑制剂，抑制hedgehog，在表达GLI1的HEK293T细胞中IC50为5 μM，选择性作用于其他通路，如TNF和糖皮质激素受体基因的转录。 |
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是一种有效的Hedgehog信号通路抑制剂。抑制肿瘤细胞的增殖和诱导其广泛性凋亡，具有抗肿瘤活性。 |
||
| S8249 |
HPI-4 (Ciliobrevin A)HPI-4 (Ciliobrevin A)是hedgehog通路的拮抗剂，抑制Shh诱导的Hh信号通路（Smo下游）的激活。 |
||
| S4747 |
JervineJervine是Hedgehog信号通路的抑制剂（IC50=500-700 nM），通过与smoothened相互作用抑制shh信号通路。 |
||
| S7160 |
Glasdegib (PF-04449913)Glasdegib（PF-04449913）是一种强效且口服生物有效的Smoothened (Smo)抑制剂，其IC50为5 nM。Phase 2。 |
||
| S1146 |
CyclopamineCyclopamine是一种特异性Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，在TM3Hh12细胞中IC50为46 nM。 |
(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 (Erismodegib, NVP-LDE225)Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。 |
RU-SKI 43 blocks Shh signaling. (a) RU-SKI 43 blocks Gli activation. NIH 3T3 cells were cotransfected with vectors encoding 8× Gli-binding site (GliBS)-Firefly luciferase (unless indicated otherwise), Renilla luciferase reporter (pRL-TK) and Shh. Confluent cells were treated with DMSO, 10 μM LDE225, 10 μM RU-SKI 43 or 10 μM C-2. The firefly luciferase (FL)/Renilla luciferase (RL) ratio in cell lysates was calculated and normalized to that measured in DMSO-treated samples; error bars represent mean ± s.d. (n = 2–3). |
|
| S2777 |
PF-5274857PF-5274857是一种有效的，选择性Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，IC50和Ki分别为5.8 nM和4.6 nM，可以穿透血脑屏障。 |
||
| S7092 |
SANT-1SANT-1直接结合到Smoothened (Smo)受体，Kd为1.2 nM，且抑制smo激动剂作用效果，IC50为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是口服生物有效的Smoothened拮抗剂。Phase 2。 |
Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).
|
|
| S3042 |
PurmorphaminePurmorphamine直接结合并激活Smoothened，阻断BODIPY-cyclopamine与Smo结合，在HEK293T细胞中IC50约为1.5 μM，也诱导成骨细胞分化，EC50为1μM |
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是一种细胞渗透性Smoothened (Smo)激动剂，其在Shh-LIGHT2细胞中的EC50约为3 nM。 |
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.
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1082 |
Vismodegib (GDC-0449)Vismodegib (GDC-0449)是一种新型有效的，特异性hedgehog抑制剂，无细胞试验中IC50为3 nM，也会抑制P-gp，IC50为3.0μM。 |
SMOΔC captured on cholesterol beads in the presence of increasing concentrations of free vismodegib or 20(S)-OHC (h). Results from one of two independent pull-down experiments are shown. |
|
| S2157 |
Taladegib (LY2940680)Taladegib (LY2940680)与Smoothened(Smo)受体结合，有效抑制Hedgehog(Hh)信号通路。Phase 1/2。 |
||
| S8075 |
GANT61GANT61是一种GLI1及GLI2诱导的转录抑制剂，抑制hedgehog，在表达GLI1的HEK293T细胞中IC50为5 μM，选择性作用于其他通路，如TNF和糖皮质激素受体基因的转录。 |
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是一种有效的Hedgehog信号通路抑制剂。抑制肿瘤细胞的增殖和诱导其广泛性凋亡，具有抗肿瘤活性。 |
||
| S8249 |
HPI-4 (Ciliobrevin A)HPI-4 (Ciliobrevin A)是hedgehog通路的拮抗剂，抑制Shh诱导的Hh信号通路（Smo下游）的激活。 |
||
| S4747 |
JervineJervine是Hedgehog信号通路的抑制剂（IC50=500-700 nM），通过与smoothened相互作用抑制shh信号通路。 |
||
| S7160 |
Glasdegib (PF-04449913)Glasdegib（PF-04449913）是一种强效且口服生物有效的Smoothened (Smo)抑制剂，其IC50为5 nM。Phase 2。 |
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S1146 |
CyclopamineCyclopamine是一种特异性Hedgehog (Hh)信号通路拮抗剂，作用于Smoothened (Smo)，在TM3Hh12细胞中IC50为46 nM。 |
(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 (Erismodegib, NVP-LDE225)Sonidegib (Erismodegib, NVP-LDE225)是一种Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，无细胞试验中IC50分别为1.3 nM (小鼠)和2.5 nM(人)。Phase 3。 |
RU-SKI 43 blocks Shh signaling. (a) RU-SKI 43 blocks Gli activation. NIH 3T3 cells were cotransfected with vectors encoding 8× Gli-binding site (GliBS)-Firefly luciferase (unless indicated otherwise), Renilla luciferase reporter (pRL-TK) and Shh. Confluent cells were treated with DMSO, 10 μM LDE225, 10 μM RU-SKI 43 or 10 μM C-2. The firefly luciferase (FL)/Renilla luciferase (RL) ratio in cell lysates was calculated and normalized to that measured in DMSO-treated samples; error bars represent mean ± s.d. (n = 2–3). |
|
| S2777 |
PF-5274857PF-5274857是一种有效的，选择性Smoothened(Smo)拮抗剂，抑制Hedgehog (Hh)信号通路，IC50和Ki分别为5.8 nM和4.6 nM，可以穿透血脑屏障。 |
||
| S7092 |
SANT-1SANT-1直接结合到Smoothened (Smo)受体，Kd为1.2 nM，且抑制smo激动剂作用效果，IC50为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是口服生物有效的Smoothened拮抗剂。Phase 2。 |
Cell viability assays performed on H1650 and H1975 cells with various concentrations of BMS-833923 (B).
|
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3042 |
PurmorphaminePurmorphamine直接结合并激活Smoothened，阻断BODIPY-cyclopamine与Smo结合，在HEK293T细胞中IC50约为1.5 μM，也诱导成骨细胞分化，EC50为1μM |
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是一种细胞渗透性Smoothened (Smo)激动剂，其在Shh-LIGHT2细胞中的EC50约为3 nM。 |
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.
|
