Hedgehog/Smoothened
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| 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 |
| S7160 | Glasdegib (PF-04449913) | <1 mg/mL | 47 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 |
| S1146 | Cyclopamine | <1 mg/mL | <1 mg/mL | 2 mg/mL |
| S2151 | Sonidegib (Erismodegib, 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 |
| S8597 | LYN-1604 | 100 mg/mL | 50 mg/mL | 100 mg/mL |
| S7779 | Smoothened Agonist (SAG) HCl | 100 mg/mL | 71 mg/mL | 40 mg/mL |
- Hedgehog/Smoothened抑制剂（15）
- 新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. |
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| 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。 |
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| S7160New |
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。 |
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| 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. |
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| 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。 |
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| 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。 |
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| 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。 |
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| 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. |
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| 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). |
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| 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。 |
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| 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 |
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| 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).
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| 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.
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| S8597New |
LYN-1604LYN-1604是一种潜在的ULK1激动剂，在MDA-MB-231细胞中IC50为1.66 μM。它能与野生型ULK1结合，Kd=291.4 nM。与突变型ULK1蛋白ULK1(Y89A)的结合亲和力急剧减小，其Kd值比ULK1、ULK1 (K50A)和ULK1 (L53A)大。 |
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| 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。 |
