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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T22414	RBN012759	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	RBN012759 是选择性和具有口服活性的 PARP14抑制剂，IC50值小于3 nM，可降低促肿瘤巨噬细胞功能并在肿瘤外植体中引发炎症反应，比对 monoPARPs 的选择性高 300 倍，比对 polyPARPs 的选择性高 1000 倍。
T37860	T 26c disodium salt
	Highly potent and selective MMP13 inhibitor (IC50 = 6.9 pM). Exhibits >2600-fold selectivity for MMP13 over related MMPs. Inhibits degradation of bovine nasal septum cartilage explants in vitro . Orally bioavailable. Nara et al (2014) Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1 binding site. Bioorg.Med.Chem. 22 5487 PMID:25192810"
T28487	Quininib
	Quininib is a regulator of Ocular Angiogenesis. Quininib significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice.
T37577	Glycogen Phosphorylase Inhibitor
	Glycogen phosphorylase in the liver, muscle, and brain initiate glycogenolysis by releasing glucose-1-phosphate from glycogen. Glycogen phosphorylase inhibitor is a cell-permeable acyl urea first identified as an inhibitor of human liver glycogen phosphorylase (IC50 = 53 nM). It blocks glucagon-induced hepatic glycogenolysis in vivo. Glycogen phosphorylase inhibitor has been used to study glycogen utilization in human liver HepG2 cells, retinal explants, and human T lymphocyte Kit 225 cells.
T70312	AZ1366
	AZ1366 is a potent tankyrase inhibitor that enhances irinotecan activity in tumors that exhibit elevated tankyrase and irinotecan resistance. Combination AZ1366 and irinotecan achieved greater anti-tumor effects compared to monotherapy. Activity was limited to CRC explants that displayed irinotecan resistance and increased protein levels of tankyrase and NuMA.
T37409	DPC-AJ1951 (trifluoroacetate salt) DPC-AJ1951 (trifluoroacetate salt)
	DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants...
T71420	RO314724
	RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants.

化合物

Glycogen Phosphorylase Inhibitor

DPC-AJ1951 (trifluoroacetate salt)

Cat.No: T37409

Synonym: DPC-AJ1951 (trifluoroacetate salt)

Cat. No.	Product Name	Target	Signaling Pathways
T4601	9-Methoxycanthin-6-one	Others	Others
	9-Methoxycanthin-6-one 是存在于完整植株和不同外植体的愈伤组织中的 Canthin-6-one 生物碱，具有抗肿瘤作用。