Hedgehog (Hh) is composed of N-terminal and C-terminal domains that dissociate in a self-catalyzed proteolytic cleavage reaction. The N-terminal product HhNp, modified by cholesterol during self-cleavage, harbors all known Hh signaling activities. When synthesized in the absence of the C-terminal domain (and hence lacking cholesterol modification), the N-terminal domain is aberrantly targeted and released selectively into the retina.
Hedgehog signaling pathway is linked to tumorigenesis and is aberrantly activated in a variety of cancers. Hh ligands bind to and suppress the transmembrane receptor Patched (PTCH), which suppresses Smoothened (SMO), a seven-transmembrane-helix protein that positively regulates the Hh pathway.
Sonic hedgehog (Shh) is a morphogen essential to the developing nervous system that continues to play an important role in adult life by contributing to cell proliferation and differentiation, maintaining blood-brain barrier integrity, and being cytoprotective against oxidative and excitotoxic stress, all features of importance in amyotrophic lateral sclerosis (ALS).
Indian hedgehog (Ihh), a signaling molecule that plays a pivotal role in the regulation of chondrocyte proliferation, maturation, and ossification both in long-bone development and digit joint formation, has also been found to be essential for temporomandibular joint (TMJ) development.
Desert hedgehog (Dhh), one of the Hedgehog family members, is expressed by Schwann cells of peripheral nerves.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PC15896 | 20(S)-Hydroxycholesterol | 516-72-3 | Hedgehog信号通路Smoothened(Smo)癌蛋白的变构激活剂,20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) 是平滑 (smo) 癌蛋白的变构激活剂,在以 NIH3T3 细胞的基因转录报告实验中,激活 hedgehog (Hh) 信号通路的 EC50 值为 3 μM。 |
PC15846 | AY 9944 dihydrochloride | 366-93-8 | Δ7固醇还原酶抑制剂,AY 9944 是一种特异的胆固醇生物合成 (cholesterol biosynthesis) 抑制剂。AY 9944 抑制 7- 脱氢胆固醇 Δ7- 还原酶 (DHCR7) 酶 (IC50=13 nM)。 |
PC15844 | Ciliobrevin A | 302803-72-1 | Hh通路拮抗剂,Ciliobrevin A 是一种 Hedgehog (Hh) 信号通路抑制剂,平均抑制浓度 (50) 值小于 10 μM。 |
PL02550 | Ciliobrevin D | 1370554-01-0 | Ciliobrevin D 是一种细胞渗透性,可逆和特异性的 AAA + ATPase 运动细胞质动力蛋白抑制剂。Ciliobrevin D 抑制 Hedgehog (Hh) 信号和初级纤毛形成。Ciliobrevin D 在体外抑制依赖于动力蛋白的微管滑动和 ATPase 活性。 |
PC15908 | CUR 61414 | 334998-36-6 | hedgehog诱导的细胞活性的强效抑制剂,CUR61414 是一种新型的可渗透细胞的 Hedgehog 信号通路抑制剂 (IC50 =100-200 nM),CUR61414 是氨基脯氨酸类化合物的小分子成员,可选择性结合 Smoothened (Smo),Ki 值为 44 nM。CUR-61414可以诱导癌细胞凋亡 (apoptosis) 而不会影响非癌症细胞。 |
PC15838 | Cyclopamine | 4449-51-8 | Hedgehog (Hh)信号抑制剂,Cyclopamine 是 Hedgehog 通路的拮抗剂,在细胞实验中的 IC50 为 46 nM。 |
PL02509 | Dynarrestin | 2222768-84-3 | Dynarrestin 是细胞质动力蛋白 1 和 2 的氨基噻唑抑制剂。Dynarrestin 快速可逆地抑制动力蛋白 1 驱动的微管在体外滑动和细胞内动力蛋白 1 和 2 依赖性过程,而不影响 ATP 水解和干扰纤毛发生。Dynarrestin 抑制神经元前体和肿瘤细胞的刺猬因子 (Hh) 依赖性增殖。 |
PL02720 | Hh-Ag1.5 | 612542-14-0 | Hh-Ag1.5 (SAg1.5) 是一种有效的 Hedgehog (Hh) 激动剂,EC50 为 1 nM。Hh-Ag1.5 介导的重编程打破了非损伤肝脏干细胞的静止状态,从而挽救了肝衰竭。 |
PC15843 | HPI 1 | 599150-20-6 | Hh信号传导抑制剂,HPI-1 is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Shh (IC50=1.5 uM) without significantly affecting Wnt signaling (IC50>30 uM). |
PL04733 | Itraconazole-d3 | 1217512-35-0 | Itraconazole-d3 是 Itraconazole (HY-17514) 的氘代物。 |
PC15845 | Jervine | 469-59-0 | Hedgehog信号抑制剂,Jervine(11-Ketocyclopamine)是甾体类生物碱,能阻断sonic hedgehog(Shh)信号通路,抑制Smo。 |
PC15841 | JK 184 | 315703-52-7 | Hh信号传导抑制剂,JK184 是一种有效的 Hedgehog (Hh) 抑制剂,在哺乳动物细胞中,IC50 为 30 nM。 |
PC15840 | LY2940680 | 1258861-20-9 | Hedgehog / SMO拮抗剂,抑制Hh信号,Taladegib (LY2940680) 是一种 smoothened 受体拮抗剂。 |
PL01022 | MK-4101 | 935273-79-3 | MK-4101 是一种 SMO 拮抗剂 (对 293 细胞的 IC50 为 1.1 µM),也是一种有效的 hedgehog 途径抑制剂 (对小鼠细胞的 IC50 为 1.5 µM;对 KYSE180 食管癌细胞的 IC50 为 1 µM)。MK-4101 具有强大的抗肿瘤活性,能抑制肿瘤细胞增殖并诱导细胞凋亡。 |
PC15907 | Oxy-16 | 596-94-1 | hedgehog活性的拮抗剂,Oxy-16 is an antagonist of hedgehog activity. |
PC15839 | PF-5274857 | 1373615-35-0 | 高效选择性Smo拮抗剂,PF-5274857是Smo拮抗剂,能抑制Hedgehog信号转导,IC50和Ki分别为5.8 nM和4.6 nM,能渗透入血脑屏障。 |
PC15881 | SAG | 912545-86-9 | Hh和Smo激动剂,SAG 是一种有效的 Smo 受体 激动剂,能够活化 Hedgehog 信号通路,Kd 值为 59 nM。 |
PC15847 | SANT-1 | 304909-07-7 | shh抑制剂,SANT-1 是一种有效的 Smo 拮抗剂,能够抑制 Hedgehog 通路,在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中,IC50 值分别为 20 nM 和 30 nM。 |
PC15842 | SANT-2 | 329196-48-7 | Hedgehog信号通路抑制剂,Inhibitor of Sonic hedgehog (Shh) signaling; antagonizes smoothened receptor activity (KD = 12 nM). |
PC15887 | U 18666A | 3039-71-2 | 胆固醇转运和合成抑制剂,U18666A,一个细胞渗透性药物,是胆固醇合成和转运的抑制剂。 |