Laduviglusib trihydrochloride,

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Laduviglusib trihydrochloride

CAS No. : 1782235-14-6

MCE 国际站：Laduviglusib trihydrochloride

产品活性：Laduviglusib (CHIR-99021) trihydrochloride 是一种有效的选择性 GSK-3α/β 抑制剂，IC₅₀ 为 10 nM 和 6.7 nM。CHIR-99021 trihydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib trihydrochloride 能诱导细胞自噬 (autophagy)。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Autophagy

作用靶点：GSK-3  |  Wnt  |  β-catenin  |  Autophagy

In Vitro: Laduviglusib trihydrochloride inhibits human GSK-3β with K_i values of 9.8 nM. Laduviglusib trihydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib trihydrochloride specifically inhibits GSK3β (IC₅₀=~5 nM) and GSK3α (IC₅₀=~10 nM), with little effect on other kinases. In the presence of Laduviglusib trihydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib trihydrochloride with an IC₅₀ of 4.9 μM.

In Vivo: In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) trihydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration. Laduviglusib (2 mg/kg) trihydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib trihydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX⁺ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride treatment increases Lgr5⁺ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h.

相关产品：Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Wnt/Hedgehog/Notch Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Alzheimer's Disease Compound Library  |  Neuroprotective Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Anti-Obesity Compound Library  |  Transcription Factor-Targeted Library  |  Glucose Metabolism Compound Library  |  Antidepressant Compound Library  |  Human Metabolite Library  |  Anti-Pulmonary Fibrosis Compound Library  |  Osteogenesis Compound Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Highly Selective Activators Library  |  Cell Death Library  |  Serine/Threonine Kinase Inhibitor Library  |  Laduviglusib  |  XAV-939  |  IWR-1  |  IWP-2  |  ICG-001  |  Wnt-C59  |  MSAB  |  SKL2001  |  SB 216763  |  Bisindolylmaleimide I  |  Heparan Sulfate  |  Kenpaullone  |  LY2090314  |  Adavivint  |  Wogonin  |  Salinomycin  |  Pyrvinium pamoate  |  GSK 3 Inhibitor IX  |  Echinacoside  |  Ceftriaxone sodium salt  |  TWS119  |  Tegatrabetan  |  BML-284  |  Tideglusib  |  AR-A014418  |  LF3  |  NCB-0846  |  iCRT3

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds