Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T22814 |
GSA-10
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
GSA-10是新型的喹啉甲酰胺衍生物,有效激动平滑受体剂,EC50为 1.2 μM。它作用于Smo,促进多能间充质干细胞分化为成骨细胞。它介导 Hedgehog 信号传导,这可能对癌症疾病的再生医学具有研究意义。 | |||
T2250 |
DY131
DY 131,GSK 9089,DY-131 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Smo | Endocrinology/Hormones; Stem Cells |
DY131 (DY-131) 是选择性的 ERRγ 和 ERRβ 激动剂,对 ERRα,ERα 和 ERβ 无效。它对Smo 的信号传导具有抑制作用。 | |||
T2666 |
Taladegib
LY2940680 |
Hedgehog/Smoothened; Smo | GPCR/G Protein; Stem Cells |
Taladegib (LY2940680) 是smoothened 受体拮抗剂。 | |||
T23027 |
MRT-10
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
MRT 10 是一种七跨膜平滑受体 (Smo) 拮抗剂,通过多种 Hedgehog (Hh) 测定,其IC50=0.65 μM。它与Smo 受体结合的位点是 Bodipycyclopamine。它可用于研究癌症。 | |||
T2450 |
SANT-1
SANT 1 |
Hedgehog/Smoothened; Smo | GPCR/G Protein; Stem Cells |
SANT-1 是Smo 拮抗剂,能够抑制Hedgehog 通路,在 Shh-LIGHT2 和 SmoA1-LIGHT2 实验中,得到的IC50值分别为 20 nM 和 30 nM。 | |||
T1779 |
SAG
Smoothened Agonist (SAG) HCl,Smoothened Agonist |
Hedgehog/Smoothened; Smo | GPCR/G Protein; Stem Cells |
SAG (Smoothened Agonist) 是一种 Smo 受体激动剂 (EC50=3 nM),具有细胞渗透性和选择性。SAG 可以直接结合 Smo 螺旋束调节 Smo 活性,可以活化 Hedgehog 信号通路。 | |||
T40465 |
SAG dihydrochloride
|
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
SAG dihydrochloride 是一种强效的 Smoothened(Smo)受体激动剂(EC 50 =3 nM;K d =59 nM)。SAG dihydrochloride 可激活刺猬信号通路并抵消环丙胺对 Smo 的抑制。 | |||
T24754 |
Hh-Ag1.5
SAG-1.5,SAG1.5,SAG 1.5 |
Hedgehog/Smoothened | GPCR/G Protein; Stem Cells |
Hh-Ag1.5 (SAG-1.5) 是一种高效的 Hedgehog (Hh) 激动剂(EC50: 1 nM)和Smoothened (Smo)受体激动剂,对Smo的 EC50 为 1 nM、 Ki值在 0.5 和 2.3 nM 之间。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。Hh-Ag1.5 诱导 hiPSCs 分化为皮肤前体细胞、脊髓运动神经元和脊髓感觉神经元。 | |||
T22958 | M 25 | Others | Others |
Smoothened (Smo) receptor antagonist | |||
T23307 |
SANT 2
SANT-2 |
Others | Others |
SANT-2 is an inhibitor of Sonic hedgehog signaling and also antagonizes smoothened receptor activity (KD = 12 nM). | |||
T71520 |
LEQ-506
|
||
LEQ506, also known as NPV-LEQ506, is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. Smoothened antagonist LEQ506 selectively binds to the Hedgehog (Hh)-ligand cell surface receptor Smo, which may result in the suppression of the Hh signaling pathway, thereby inhibiting tumor cell growth. | |||
T38767 |
MRT-83 hydrochloride
|
||
MRT-83 (hydrochloride) is a potent antagonist of the Smoothened (Smo) receptor, effectively inhibiting the Hedgehog (Hh) signaling pathway and BODIPY-cyclopamine binding to human Smo. With its potential applications in the study of cancer disease, MRT-83 (hydrochloride) demonstrates promising prospects for research purposes. | |||
T70693 | MRT-92 HCl salt | ||
MRT-92 is a potent and selective Smoothened (Smo) receptor inhibitor. MRT-92 displays subnanomolar antagonist activity against Smo in various Hh cell-based assays. MRT-92 inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation through pharmacologic (half maximal inhibitory concentration [IC50] = 0.4 nM) or genetic manipulation. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain. | |||
T35562 |
Nat-20(S)-yne
|
||
Smoothened (SMO) is a GPCR-like receptor which, with Patched, mediates hedgehog signaling to regulate gene expression through the Gli transcription factors. 20(S)-hydroxy Cholesterol (20(S)-OHC) is an oxysterol which binds SMO and activates hedgehog signaling (EC50 = 3 μM), and this activation is selective for the nat-20(S)-OHC enantiomer. Nat-20(S)-OHC synergizes with the SMO agonist SAG, suggesting an allosteric effect. Nat-20(S)-yne is a form of nat-20(S)-OHC with a terminal alkyne group, whi... | |||
T83910 |
S1PL-IN-31
Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31 |
||
S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM),同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内,S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中,由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平,并且在雌性大鼠中降低了心率。 |