Dorsomorphin (Compound C)

For research use only.

Catalog No.S7840 Synonyms: BML-275,Compound C

301 publications

Dorsomorphin (Compound C) Chemical Structure

CAS No. 866405-64-3

Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.

Selleck's Dorsomorphin (Compound C) has been cited by 301 publications

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Biological Activity

Description Dorsomorphin (Compound C, BML-275) is a potent, reversible, selective AMPK inhibitor with Ki of 109 nM in cell-free assays, exhibiting no significant inhibition of several structurally related kinases including ZAPK, SYK, PKCθ, PKA, and JAK3. Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6. Dorsomorphin is used in promoting specific cell differentiation and inducing cancer cell line autophagy. For animal testing, the water-soluble S7306 Dorsomorphin (Compound C) 2HCl is recommended.
Targets
ALK2 [3]
()
ALK3 [3]
()
ALK6 [3]
()
AMPK [1]
(Cell-free assay)
109 nM(Ki)
In vitro

Dorsomorphin inhibits ACC inactivation by either AICAR or metformin, and also attenuates AICAR and metformin’s effect to increase fatty acid oxidation or suppress lipogenic genes in hepatocytes. [1] Inhibition of AMPK activity by Dorsomorphin almost completely inhibits autophagic proteolysis in HT-29 cells. [2] in addition, Dorsomorphin selectively inhibits the BMP type I receptors ALK2, ALK3 and ALK6, and thus blocks BMP-mediated SMAD1/5/8 phosphorylation, target gene transcription and osteogenic differentiation. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
C2C12 NYT5S5MzTnWwY4Tpc44h[XO|YYm= M3zlclQhfU1? MVPJcohq[mm2aX;uJI9nKEKPUGKxMY1m\GmjdHXkJI9{fGWxYnzhd5Qh\GmoZnXy[Y51cWG2aX;uJIlvKEKPUEStd5RqdXWuYYTl[EBud3W|ZTDDNmMyOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDhcItidGmwZTDwbI9{eGijdHHz[UBt\X[nbDDheEA1KHWPIHL5JJNx\WO2cn;wbI91d22ndIL5 MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDB{NkC5OEc,OThyMk[wPVQ9N2F-
C2C12 MUXGeY5kfGmxbjDhd5NigQ>? MmfaOEB2VQ>? M1nXVWlvcGmkaYTpc44hd2ZiQl3QVlEudWWmaXH0[YQhd3O2ZX;icIF{fCCmaX\m[ZJmdnSrYYTpc44hcW5iQl3QOk1{fGmvdXzheIVlKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJIFtc2GuaX7lJJBpd3OyaHH0ZZNmKGyndnXsJIF1KDRidV2gZpkhe3CnY4Tyc5Bpd3SxbXX0dpk> NHrERnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECyOlA6PCd-MUiwNlYxQTR:L3G+
HepG2 MV7GeY5kfGmxbjDhd5NigQ>? Ml6yNVAhfU1? NXXQV2ZmOzBibXnudy=> NEX2NmVKdmirYnn0bY9vKG:oIFLNVHIyNW2nZHnheIVlKGincHPp[IlvKG2UTlGg[ZhxemW|c3nvckBqdiCETWCyMZN1cW23bHH0[YQhcHWvYX6gTIVxTzJiY3XscJMh[XRiMUCgeW0hfHKnYYTl[EA{OCCvaX7zJIJm\m:{ZTDCUXAzKGOqYXzs[Y5o\SCvZXHzeZJm\CCjZoTldkAyPiCqcoOgZpkheVKWLWDDVkBidmGueYPpdy=> NXfnZ|htRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNlYxQTRpPkG4NFI3ODl2PD;hQi=>
Hep3B M4TNTmZ2dmO2aX;uJIF{e2G7 NV7ZToh[OTBidV2= MkO0N|AhdWmwcx?= MWfJcohq[mm2aX;uJI9nKEKPUGKxMY1m\GmjdHXkJIhmeGOrZHnuJI1TVkFiZYjwdoV{e2mxbjDpckBKVDZvc4TpcZVt[XSnZDDoeY1idiCKZYCzRkBk\WyuczDheEAyOCC3TTD0doVifGWmIEOwJI1qdnNiYnXmc5JmKEmONjDjbIFtdGWwZ3WgcYVie3W{ZXSgZYZ1\XJiNjDodpMh[nlicWLUMXBEWiCjbnHsfZNqew>? M1i4SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEK2NFk1Lz5zOECyOlA6PDxxYU6=
Hep3B NEmxd29HfW6ldHnvckBie3OjeR?= NGjkeI4yOCC3TR?= NYHhfIxVOzBibXnudy=> NXLTO2ZDUW6qaXLpeIlwdiCxZjDCUXBTOS2vZXTpZZRm\CCLZEGgcXJPSSCneIDy[ZN{cW:wIHnuJGlNPi2|dHnteYxifGWmIHj1cYFvKEincEPCJINmdGy|IHH0JFExKHWPIITy[YF1\WRiM{CgcYlveyCkZX\vdoUhUUx4IHPoZYxt\W6pZTDt[YF{fXKnZDDh[pRmeiB4IHjyd{BjgSCzUmStVGNTKGGwYXz5d4l{ MkGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOThyMk[wPVQoRjF6MEK2NFk1RC:jPh?=
A673 M3m0W5FJXFNiYYPzZZk> M{LLT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| MoS1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY NILoSFRyUFSVIHHzd4F6 NF;xemxyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NXv5e4V5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 M3HMWJFJXFNiYYPzZZk> M1\YRZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD MWrxTHRUKGG|c3H5 MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MXTxTHRUKGG|c3H5 MVLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NFTXZ2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 NWnWXYFyeUiWUzDhd5NigQ>? MWXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) MXHxTHRUKGG|c3H5 NGXR[mFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= NXi4[XZ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M2rMdZFJXFNiYYPzZZk> NEnKT4RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 M4e5XJFJXFNiYYPzZZk> NYOw[Fl7eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> Mn\pQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NF7WWYJyUFSVIHHzd4F6 MU\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MVnxTHRUKGG|c3H5 MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh|MDDj[Yxtew>? NG\YfXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MmLwdWhVWyCjc4PhfS=> NYjGWmJpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M3XJR5FJXFNiYYPzZZk> MnfPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NGPJOWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M1y2TpFJXFNiYYPzZZk> NYWwU|hEeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NGLtTFdyUFSVIHHzd4F6 NVvo[|lZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NEHZbYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MYXxTHRUKGG|c3H5 MnzHdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NHTlRYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Id1 / Id2 / Id3 ; 

PubMed: 25010525     


Dorsomorphin dramatically inhibited the expression of Ids. KMM cells were treated with 5 µM Dorsomorphin for 24 hours before harvesting. Expressions of Ids were detected by immunoblotting. 

pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α; 

PubMed: 29531259     


PC-3 and LNCaP cells were treated with vehicle, 25 µM compound 8c, 25 µM compound 8c + 5 μM Dorsomorphin (8c + D) or 5 μM Dorsomorphin (D), for 1 hour or 24 hours and levels of the phosphorylated AMPK (pAMPK), phosphorylated ACC (pACC), phosphorylated Raptor (pRaptor) forms and HIF1α were determined by Western blot. Upper panel, representative Western blot of three different experiments. β-tubulin (β-Tub) serves as a loading control. Lower panel, densitometric analyses of bands represented as the mean of the ratio pAMPK/AMPK or pACC/ACC. 

25010525 29531259
Immunofluorescence
p-AMPK / Sirt1 / p66Shc ; 

PubMed: 28728079     


Cellular immunofluorescence with anti-p-AMPK, anti-Sirt1 and anti-p66Shc antibodies. High levels of p-AMPK were observed under LG conditions and were accompanied by Sirt1 expression. HG reduced this fluorescence. This effect was reversed by probucol treatment and Dorsomorphin and EX-527 treatment but was increased by AICAR treatment. Contrasting results were observed regarding p66Shc and DHE staining (lower panel). 

28728079
In vivo Dorsomorphin (10 mg/kg) reduces basal levels of hepcidin expression and increases serum iron concentrations in adult mice. [3] Dorsomorphin (0.2 mg/kg, i.v.) significantly reduces VCAM-1 and ICAM-1 expression in the thoracic aorta of LPS-treated rats. [4]

Protocol

Animal Research:[3]
- Collapse
  • Animal Models: Iron-replete mice
  • Dosages: ~10 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL warmed (2.5 mM)
Water Insoluble
Ethanol '''''2 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 399.49
Formula

C24H25N5O

CAS No. 866405-64-3
Storage powder
in solvent
Synonyms BML-275,Compound C
Smiles C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID