gli1

GANT 61 (GANT61) 是一种Gli1和Gli2抑制剂，靶向Hedgehog GLi 通路。

GLI1-IN-1 (CBC-1)，一种GLI-1抑制剂，展现出优异的水溶性及抗癌特性。该化合物能通过抑制Hedgehog (HH) 通路 (IC50=1.3 μM) 来阻止结直肠癌的生长，并能诱导细胞凋亡 (apoptosis)。

Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。

HhAntag 是高效的、特异性的、具有口服活性的 Hh 通路的SMO 拮抗剂。

Prostaglandin E1 ethanolamide，前列腺素E1 (PGE1) 的类似物，可能有效抑制GLI2诱导的靶基因表达（包括Gli1和Ptch1）和肿瘤生长。

Jervine (Jerwiny) 是一种有效的刺猬 (Hh) 抑制剂(IC50:500-700 nM)。它是一种天然致畸性甾体生物碱，来自于 Veratrumalbum 的根茎，具有抗炎和抗氧化作用。

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

GANT 58 (NSC-75503) 是GLI 拮抗剂，能够抑制 GLI1 诱导的转录，其IC50=5 μM。

Robotnikinin is an Shh signaling inhibitor in a concentration-dependent manner. It acts by exhibiting significant repression of Shh-induced Gli1/Gli2.

Glabrescione B is a novel compound that specifically binds to Gli1, an important modulator of the Hedgehog (Hh) signaling pathway. By disrupting the Gli1-DNA interaction, Glabrescione B effectively impairs the activity of Gli1. Moreover, Glabrescione B demonstrates potent inhibitory effects on the growth of tumor cells that rely on Hedgehog signaling, as well as on the self-renewal capacity and clonogenicity of tumor-derived stem cells.

Physalin H is an Hh signaling inhibitor blocks GLI1-DNA-complex formation, it also strong quinone reductase induction activity with IR (Induction ratio, QR induction activity) value of 3.74±0.02. Physalin H shows immunosuppressive effects on T cells both

TPB15 是一种口服具有活力的 Hh(Hedgehog) 信号抑制剂。TPB15 可以明显阻滞 MDA-MB-468 细胞周期，并诱导其凋亡。TPB15 阻断 Smo(Smoothened) 转位到纤毛中，减少 Smo 蛋白和 mRNA 表达。TPB15 对下游调控因子胶质瘤相关癌基因1 (Gli1) 的表达表现出抑制作用。TPB15 具有较好的抗肿瘤作用，且毒性较低。

TAK-441 是一种具有口服活性的 Hedgehog 信号抑制剂 (IC50 = 4.4 nM)，具有有效的抗肿瘤活性。 TAK-441 抑制转录因子 Gli1 mRNA 表达和肿瘤生长。

Physalin A 是一种从 P. alkekengi 中分离的抗炎化合物，具有抗纤维化作用，通过 ERK 和 p38 调节 Nrf2 通路以诱导解毒酶。 Physalin A 阻断 NF-kappaB 信号通路的激活。Physalin A 通过降低 GLI1 基因和 YAP1 基因的表达来减少乳腺球的形成。

HSP70-IN-3 是一种有效的热休克蛋白 (HSP70) 抑制剂 (ASZ001 和 C3H10T1 2 的 IC50分别为1.1和1.9 μM)。HSP70-IN-3 具有抗 Hedgehog 信号转导通路活性和抗增殖活性，并降低致癌转录因子 GLI1 的表达。

HPI 1 是一种刺猬 (Hh) 信号抑制剂。在 Shh-LIGHT2 细胞中抑制 Sonic Hedgehog (Shh)-、SAG- 和 Gli 诱导的 Hh 通路激活（Shh-、SAG-、Gli2- 和 Gli1 诱导的激活的 IC50 值为 1.5、1.5、4 和 6 μM） .

MS-0022 is a SMO antagonist. MS-0022 showed effective Hh signaling pathway inhibition at the level of SMO in the low nM range, and Hh pathway inhibition downstream of Suppressor of fused (SUFU) in the low µM range. MS-0022 reduced growth in the tumor cell lines PANC-1, SUIT-2, PC-3 and FEMX in vitro. MS-0022 is a treatment led to a transient delay of tumor growth that correlated with a reduction of stromal Gli1 levels in SUIT-2 xenografts in vivo.