Dorsomorphin (Compound C) 2HCl

Catalog No.S7306 Synonyms: BML-275 2HCl,Compound C 2HCl

For research use only.

Dorsomorphin 2HCl (BML-275, Compound C) 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. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.

Dorsomorphin (Compound C) 2HCl Chemical Structure

CAS No. 1219168-18-9

Selleck's Dorsomorphin (Compound C) 2HCl has been cited by 432 publications

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Biological Activity

Description Dorsomorphin 2HCl (BML-275, Compound C) 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. Also inhibits type Ⅰ BMP receptor activity. Dorsomorphin induces autophagy in cancer cell line.
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 Mn2ySpVv[3Srb36gZZN{[Xl? MWG0JJVO M2iwZ2lvcGmkaYTpc44hd2ZiQl3QVlEudWWmaXH0[YQhd3O2ZX;icIF{fCCmaX\m[ZJmdnSrYYTpc44hcW5iQl3QOE1{fGmvdXzheIVlKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJIFtc2GuaX7lJJBpd3OyaHH0ZZNmKGyndnXsJIF1KDRidV2gZpkhe3CnY4Tyc5Bpd3SxbXX0dpk> NVTjVJk1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUiwNlYxQTRpPkG4NFI3ODl2PD;hQi=>
C2C12 NFHaRo5HfW6ldHnvckBie3OjeR?= Mln3OEB2VQ>? M{\rNGlvcGmkaYTpc44hd2ZiQl3QVlEudWWmaXH0[YQhd3O2ZX;icIF{fCCmaX\m[ZJmdnSrYYTpc44hcW5iQl3QOk1{fGmvdXzheIVlKG2xdYPlJGMzSzF{IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJIFtc2GuaX7lJJBpd3OyaHH0ZZNmKGyndnXsJIF1KDRidV2gZpkhe3CnY4Tyc5Bpd3SxbXX0dpk> NE\GTpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECyOlA6PCd-MUiwNlYxQTR:L3G+
HepG2 MVvGeY5kfGmxbjDhd5NigQ>? NWe1Z3J3OTBidV2= MXezNEBucW6| MU\Jcohq[mm2aX;uJI9nKEKPUGKxMY1m\GmjdHXkJIhmeGOrZHnuJI1TVkFiZYjwdoV{e2mxbjDpckBDVVB{LYP0bY12dGG2ZXSgbJVu[W5iSHXwS|Ih[2WubIOgZZQhOTBidV2geJJm[XSnZDCzNEBucW6|IHLl[o9z\SCETWCyJINp[WyuZX7n[UBu\WG|dYLl[EBi\nSncjCxOkBpenNiYomgdXJVNVCFUjDhcoFtgXOrcx?= M1Xqb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6MEK2NFk1Lz5zOECyOlA6PDxxYU6=
Hep3B NILIb4pHfW6ldHnvckBie3OjeR?= NVnOTpU3OTBidV2= NGLCT4M{OCCvaX7z M125U2lvcGmkaYTpc44hd2ZiQl3QVlEudWWmaXH0[YQhcGWyY3nkbY4hdVKQQTDlfJBz\XO|aX;uJIlvKEmONj3zeIlufWyjdHXkJIh2dWGwIFjldFNDKGOnbHzzJIF1KDFyIIXNJJRz\WG2ZXSgN|AhdWmwczDi[YZwemViSVy2JINp[WyuZX7n[UBu\WG|dYLl[EBi\nSncjC2JIhzeyCkeTDxVnQuWEOUIHHuZYx6e2m| NHGx[ZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECyOlA6PCd-MUiwNlYxQTR:L3G+
Hep3B MUTGeY5kfGmxbjDhd5NigQ>? MUGxNEB2VQ>? M3LC[VMxKG2rboO= NGPiNnVKdmirYnn0bY9vKG:oIFLNVHIyNW2nZHnheIVlKEmmMTDtVm5CKGW6cILld5Nqd25iaX6gTWw3NXO2aX31cIF1\WRiaIXtZY4hUGWyM1KgZ4VtdHNiYYSgNVAhfU1idILlZZRm\CB|MDDtbY5{KGKnZn;y[UBKVDZiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDZiaILzJIJ6KHGUVD3QR3Ih[W6jbInzbZM> NGnrV3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOECyOlA6PCd-MUiwNlYxQTR:L3G+
A673 NY\qUVV1eUiWUzDhd5NigQ>? MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NVzwOIg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY MYTxTHRUKGG|c3H5 NIjZfHNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= NEHmZlQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 NHjGXVlyUFSVIHHzd4F6 NEm1[m9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= MkfEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD NFnnS4hyUFSVIHHzd4F6 M33OS5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>? MkPLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH MorFdWhVWyCjc4PhfS=> MnrQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 MYjxTHRUKGG|c3H5 NGX6PINyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MmTVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NVXTOZdyeUiWUzDhd5NigQ>? NXPYeY9oeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NFvMPYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MYfxTHRUKGG|c3H5 M2jXZpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= M{PnNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 M4L5cpFJXFNiYYPzZZk> NF22em1yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NVzncIVSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 MYrxTHRUKGG|c3H5 NG\acnJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= Mn3iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 NF[4d5JyUFSVIHHzd4F6 NX;JV4Y6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoN|Ah[2WubIO= NID0Z3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 MojNdWhVWyCjc4PhfS=> MlfMdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= MoTMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NE[4c5hyUFSVIHHzd4F6 NGjFOIZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NH[yVoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 MmXVdWhVWyCjc4PhfS=> NHfucpZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NUe2XGlwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NWPhXmFGeUiWUzDhd5NigQ>? M4CycZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= M1z1d|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 Mme1dWhVWyCjc4PhfS=> NXPPNJV3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= MnHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
KB-3-1 NInzWW9yUFSVIHHzd4F6 NU[0d4VNWC2pbInjc5Bzd3SnaX6gd5Vje3S{YYTld{Bq\GWwdHnmbYVlKGmwIFvCMVMuOSCjZHXuc4NiemOrbn;tZUBk\WyuIHzpcoUtKHGKVGOgeIhmemGyZYX0bYMhdGmkcnHyfUB{[3KnZX6= M3zPblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
Assay
Methods Test Index PMID
Western blot p-SMAD / SMAD ; Id1 / Id2 / Id3 ; pAMPK / AMPK / pACC / ACC / pRaptor / HIF1α ; p-ERK / ERK / Bcl2 / BAX / Cleaved caspase-3 ; LC3B I/ LC3B II 30808965 25010525 29531259 30155931
Immunofluorescence MyHC ; Id1 / MyoD 20689554
Growth inhibition assay Cell viability (MM cells) ; Cell viability (glioma cell lines) 25010525 24419061
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 (from reference)

Animal Research:[3]
  • Animal Models: Iron-replete mice
  • Dosages: ~10 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
PBS
For best results, use promptly after mixing.

15mg/mL

Chemical Information

Molecular Weight 472.41
Formula

C24H25N5O.2HCl

CAS No. 1219168-18-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
Is there any information you may provide as to WHICH AMPK SUBUNIT is this drug targeting in the AMPK complex?

Answer:
According to the reference (see link below), Dorsomorphin(Compound C) should target the AMPK alpha subunit through ALCAR or metformin. http://www.ncbi.nlm.nih.gov/pubmed/20844250

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