smoothened receptor

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。

Halcinonide (Halciderm) 是一种糖皮质激素，可用于局部皮肤感染的研究。

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。

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。

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。

MRT-92 是一种针对Smoothened(Smo)的拮抗剂，具备抗癌特性 (Ki=0.7 nM)。其作用机理主要是通过阻断Smoothened受体跨膜域的重叠结合位点，抑制Hedgehog信号通路，进而影响啮齿动物小脑颗粒细胞的增殖 (IC50=0.4 nM)。该化合物广泛应用于小脑神经胶质瘤的科研领域。

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。

Smoothened (Smo) receptor antagonist

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。

Taladegib (LY2940680) 是smoothened 受体拮抗剂。

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, which can be used in linking reactions known as click chemistry. Click chemistry involves highly dependable and specific azide-alkyne bioconjugation reactions and can be used to capture or immobilize bioactive molecules. Thus, nat-20(S)-yne has been conjugated with magnetic beads to demonstrate that nat-20(S)-OHC directly binds SMO.

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.

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。

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.

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.

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。

(Rac)-SAG, an isoform of SAG, is a potent Smoothened (Smo) receptor agonist (EC₅₀ = 3 nM; Kd = 59 nM) that activates the Hedgehog signaling pathway and counteracts Cyclopamine's inhibition of Smo [1] [2] [3].