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本试剂(6-[4-[2-(1-啶哌基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶)
仅供科研实验使用,不得用于其他用途!
简介:
货 号:LC1-D-3197
名 称:6-[4-[2-(1-啶哌基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶
别 名:Dorsomorphin Free Base
C A S :866405-64-3
分子量:399.49
分子式:C24H25N5O
纯 度:HPLC/TLC:>99%
说 明:Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A.
文 献:Inhibition of bone morphogenetic protein (BMP) signaling by dorsomorphin during the early critical stage of differentiation of pluripotent embryonic stem (ES) cells promoted the development of the cardiomyocyte lineage, but at the expense of reduced differentiation of endothelial, smooth muscle, and hematopoietic cells. Hao, J., et al. "Dorsomorphin, a selective small molecule inhibitor of BMP signaling, promotes cardiomyogenesis in embryonic stem cells." PLoS One 3: e2904 (2008).Dorsomorphin disrupted zebrafish angiogenesis, but not by blocking bone morphogenic protein (BMP) signaling. Dorsomorphin also showed significant "off-target" effects against the vascular endothelial growth factor (VEGF) pathway. Hao, J., et al. "In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors." ACS. Chem. Biol. 5: 245-253 (2010).Dorsomorphin reduced phosphorylation levels of SMAD1/5/8 in cells stimulated by BMP2, BMP4, BMP6, and BMP7 selectively, and blocked BMP-, hemojuvelin-, and interleukin 6-mediated hepcidin gene transcription and BMP-induced osteogenic differentiation. It also inhibited hepcidin transcription in iron-stimulated zebrafish and induced hyperferremia in iron-replete mice. Yu, P.B., et al. "Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism." Nat. Chem. Biol. 4: 33-41 (2008).The addition of dorsomorphin to the culture medium before treatment with differentiation inducers reduced lipid accumulation in 3T3-L1 cells. Suenaga, M., et al. "BMP Inhibition with dorsomorphin limits adipogenic potential of preadipocytes." J. Vet. Med. Sci. 72: 373-377 (2010).Dorsomorphin treatment of MCF7 breast carcinoma cells led to Bax redistribution from the cytoplasm to mitochondria and caused apoptosis at least partly by ceramide upregulation, and probably not by AMPK inhibition. Jin, J., et al. "AMPK inhibitor Compound C stimulates ceramide production and promotes Bax redistribution and apoptosis in MCF7 breast carcinoma cells." J. Lipid Res. 50: 2389-2397 (2009).Insulin did not affect glucose transport in control cells but increased glucose uptake for serum-starved cells that was preventable by dorsomorphin. Ching, J.K., et al. "A role for AMPK in increased insulin action after serum starvation." Am. J. Physiol. Cell Physiol. 299: C1171-C1179 (2010).Dorsomorphin inhibited the growth of four colorectal cancer cell lines, caused G2/M arrest, and induced apoptotic or autophagic death. Yang, W.L., et al. "AMPK inhibitor compound C suppresses cell proliferation by induction of apoptosis and autophagy in human colorectal cancer cells." J. Surg. Oncol. 106: 680-688 (2012).
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