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9

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T1748 Kartogenin

KGN

TGF-beta/Smad Stem Cells
Kartogenin (KGN) 是一种人间充质干细胞分化为软骨细胞的诱导剂(EC50:100 nM)。它能够结合纤维蛋白 A,破坏其与转录因子核心结合因子 β 亚基 (CBFβ) 的相互作用,并通过调节 CBFβ-RUNX1 转录程序,诱导软骨形成,可用于研究骨关节炎。
T9138 Indirubin-3′-oxime

Indirubin-3'-monoxime

GSK-3; CDK; JNK Cell Cycle/Checkpoint; MAPK; PI3K/Akt/mTOR signaling; Stem Cells
Indirubin-3′-oxime 是一种有效的细胞周期蛋白依赖性蛋白激酶抑制剂,是 indirubin 的合成衍生物。它可通过激活软骨细胞中的 Wnt/β-catenin 信号来促进身高增长,可能在阿尔茨海默病的神经元凋亡中发挥作用。
TQ0228 Derazantinib

ARQ-087

FGFR Angiogenesis; Tyrosine Kinase/Adaptors
Derazantinib (ARQ-087) 是一种有效的,ATP 竞争型的,具有口服活性的酪氨酸激酶抑制剂,能够抑制软骨细胞FGFR1 (IC50:4.5 nM)、FGFR2 (IC50:1.8 nM)、FGFR3 (IC50:4.35nM)。
T40795 BNTA

Reactive Oxygen Species Immunology/Inflammation; Metabolism; NF-κB
BNTA 是一种有效的细胞外基质 (ECM) 调节剂。在大鼠关节炎模型中,BNTA 通过诱导超氧化物歧化酶 3 (SOD3) 促进软骨细胞上软骨结构分子的合成和超氧阴离子消除调节软骨生成从而调节关节炎。
T39531 RAD16-I hydrochloride

RAD16-I hydrochloride

RAD16-I hydrochloride is a self-assembling peptide with nanofibrous morphology that provides an optimal microenvironment for the proliferation and differentiation of human mesenchymal stem cells (hMSC) into chondrocytes. This peptide, known as RAD16-I, has been extensively studied and serves as a model to assess the amyloid-like staining properties of self-assembling peptide nanofibers (SAPNFs).
T76277L Vosoritide acetate

Vosoritide (BMN 111) acetate,一种NPR2(利尿钠肽受体2)激动剂,作用于软骨细胞增殖与分化,促进骨骼生长。
T10997 Derazantinib Racemate

ARQ-087 Racemate

Others Others
Derazantinib Racemate (ARQ-087 Racemate) 是 Derazantinib 的外消旋体。Derazantinib 是一种有效的,ATP 竞争型的,具有口服活性的酪氨酸激酶抑制剂,能够抑制软骨细胞 FGFR1 (IC50:4.5 nM)、FGFR2 (IC50:1.8 nM)、FGFR3 (IC50:4.5nM)。
T71525 AB05831

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. ...
T83733 TIP39 (human, bovine) TFA

Tuberoinfundibular Peptide of 39 Residues

TIP39作为一种神经肽及甲状旁腺激素受体2型(PTH2R)激动剂,在表达重组人或大鼠PTH2R的COS-7细胞中诱导cAMP积累(EC50分别为0.5和0.8 nM),以及在内源性表达PTH2R的F-11细胞中(EC50 = 1.15 nM)。在CFK2大鼠软骨细胞中,TIP39 (1 nM)诱导细胞周期在G0/G1阶段停滞,并减少软骨分化的主要调控因子Sox9的表达。此外,TIP39 (100 pmol/动物)在小鼠强迫游泳测试中减少了不动时间。

化合物

Kartogenin
Cat.No: T1748
Synonym: KGN
Target: TGF-beta/Smad
Indirubin-3′-oxime
Cat.No: T9138
Synonym: Indirubin-3'-monoxime
Target: GSK-3, CDK, JNK
Derazantinib
Cat.No: TQ0228
Synonym: ARQ-087
Target: FGFR
BNTA
Cat.No: T40795
Synonym:
Target: Reactive Oxygen Species
RAD16-I hydrochloride
Cat.No: T39531
Synonym: RAD16-I hydrochloride
Target:
Vosoritide acetate
Cat.No: T76277L
Synonym:
Target:
Derazantinib Racemate
Cat.No: T10997
Synonym: ARQ-087 Racemate
Target: Others
AB05831
Cat.No: T71525
Synonym:
Target:
TIP39 (human, bovine) TFA
Cat.No: T83733
Synonym: Tuberoinfundibular Peptide of 39 Residues
Target:
Cat. No. Product Name Target Signaling Pathways
T2795 Amygdalin

苦杏仁苷,Laetrile

Others Others
Amygdalin (Laetrile) 是一种植物葡萄糖苷,分离自蔷薇果实的果核中,如杏,桃,杏仁,樱桃和李子。
T6S1579 Monotropein

水晶兰苷,Monotropeine

Others Others
Monotropein (Monotropeine) 是从Morinda officinalis 中获得,能够抑制硫酸葡聚糖硫酸钠诱导的结肠炎小鼠模型中炎性因子的表达。
TN5171 Tricetin

Apoptosis; Others; Nrf2 Apoptosis; Immunology/Inflammation; Others
Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用(PPI)的强效竞争性抑制剂,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路,保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1(PS-1)表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症,保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。

天然产物

Amygdalin
Cat.No: T2795
Synonym: 苦杏仁苷,Laetrile
Target: Others
Monotropein
Cat.No: T6S1579
Synonym: 水晶兰苷,Monotropeine
Target: Others
Tricetin
Cat.No: TN5171
Synonym:
Target: Apoptosis, Others, Nrf2
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