D-3197 Dorsomorphin, Free Base, >99%

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A.

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• Dorsomorphin, also known as compound C, is a potent, reversible, ATP-competitive AMP-activated protein kinase (AMPK) inhibitor with Ki of 109 nM in the absence of AMP. Zhou, G., et al. "Role of AMP-activated protein kinase in mechanism of metformin action." J. Clin. Invest. 108: 1167-1174 (2001).
• This research compound is the free base form of dorsomorphin. We also plan to offer the dihydrochloride salt form, please inquire for availablity.
• 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).
• This dorsomorphin product is the free base form, whose CAS number is given above. The CAS number of the dihydrochloride salt form is 1219168-18-9.
• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.