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Dorsomorphin 2HCl

Name: Dorsomorphin 2HCl
Brand: Selleck Chemicals
SKU: S7306
Rating: 5 (503 reviews)

Synonyms: BML-275 2HCl,Compound C 2HCl

Catalog No.S7306 Purity:99.98%

Dorsomorphin 2HCl is a potent, reversible, selective AMPK inhibitor with K_i 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 2HCl Chemical Structure

CAS No. 1219168-18-9

Purity & Quality Control

Batch: Purity: 99.98%

99.98

Dorsomorphin 2HCl Related Products

Related Targets	AMPK-related protein kinase	Click to Expand
Related Products	Dorsomorphin AICAR (Acadesine) A-769662 GSK621 WZ4003 ex229 (compound 991) Phenformin HCl HTH-01-015 BAY-3827 O-304 MK-3903 BAM 15 Danthron	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

AMPK Signaling Pathway

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
C2C12	Function assay	4 uM		Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry	18026094
C2C12	Function assay	4 uM		Inhibition of BMPR1-mediated osteoblast differentiation in BMP6-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry	18026094
HepG2	Function assay	10 uM	30 mins	Inhibition of BMPR1-mediated hepcidin mRNA expression in BMP2-stimulated human HepG2 cells at 10 uM treated 30 mins before BMP2 challenge measured after 16 hrs by qRT-PCR analysis	18026094
Hep3B	Function assay	10 uM	30 mins	Inhibition of BMPR1-mediated hepcidin mRNA expression in IL6-stimulated human Hep3B cells at 10 uM treated 30 mins before IL6 challenge measured after 6 hrs by qRT-PCR analysis	18026094
Hep3B	Function assay	10 uM	30 mins	Inhibition of BMPR1-mediated Id1 mRNA expression in IL6-stimulated human Hep3B cells at 10 uM treated 30 mins before IL6 challenge measured after 6 hrs by qRT-PCR analysis	18026094
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
KB-3-1	qHTS assay			P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	31515284
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

ALK2 ^[3]	ALK3 ^[3]	ALK6 ^[3]	AMPK ^[1] (Cell-free assay)
			109 nM(Ki)

In vitro
In vitro	Dorsomorphin inhibits ACC inactivation by AICAR, and also attenuates AICAR’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]
Kinase Assay	AMPK partial purification and in vitro kinase assay.
Kinase Assay	Liver AMPK is partially purified from male SD rats to the blue-Sepharose step. The 100-μl reaction mixture contains 100 μM AMP, 100 μM ATP (0.5 μCi ³³P-ATP per reaction), and 50 μM SAMS in a buffer (40 mM HEPES, pH 7.0, 80 mM NaCl, 0.8 mM EDTA, 5 mM MgCl₂, 0.025% BSA, and 0.8 mM DTT). The reaction is initiated with addition of the enzyme. After 30-minute incubation at 30°C, the reaction is stopped by addition of 80 μl 1% H₃PO₄. Aliquots (100 μl) are transferred to 96-well MultiScreen plates. The plate is washed three times with 1% H3PO4 followed by detection in a Top-count. The in vitro AMPK inhibition data obtained with compound C — (6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine — are fit to the following equation for competitive inhibition by nonlinear regression using a least-squares Marquardt algorithm in a computer program written by N. Thornberry of Merck Research Laboratories: Vi/Vo = (K_m + S)/[S + K_m × (1 + I/K_i)], where Vi is the inhibited velocity, Vo is the initial velocity, S is the substrate (ATP) concentration, K_m is the Michaelis constant for ATP, I is the inhibitor (compound C) concentration, and K_i is the dissociation constant for compound C.
Cell Research	Cell lines	NIH3T3 cells
	Concentrations	10 μM
	Incubation Time	3 days
	Method	Cells were treated with hydrogen peroxide and incubated in complete medium with or without treatment with the AMPK activators, AICAR (10 μM), alone or plus AMPK inhibitor Compound C (CC, 10 μM) for 3 days.
Experimental Result Images	Methods	Biomarkers	Images	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
	Immunofluorescence	MyHC Id1 / MyoD		20689554
	Growth inhibition assay	Cell viability (MM cells) Cell viability (glioma cell lines)		25010525

In Vivo
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]
Animal Research	Animal Models	Iron-replete mice
	Dosages	~10 mg/kg
	Administration	i.v.

References

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Chemical Information & Solubility

Molecular Weight	472.41	Formula	C₂₄H₂₅N₅O.2HCl
CAS No.	1219168-18-9	SDF	Download Dorsomorphin 2HCl SDF
Smiles	C1CCN(CC1)CCOC2=CC=C(C=C2)C3=CN4C(=C(C=N4)C5=CC=NC=C5)N=C3.Cl.Cl
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

Water : 47 mg/mL

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	saline	47.000mg/ml (99.49mM)	Taking the 1 mL working solution as an example, add 47 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (21.17mM)	Taking the 1 mL working solution as an example, take 10 mg of this product and add it to 1 ml of Saline (0.9% Nacl solution), and mix evenly to make it a uniform suspension. The mixed solution should be used immediately for optimal results.
Clear solution	saline	94.000mg/ml (198.98mM)	Taking the 1 mL working solution as an example, add 94 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	saline	94.000mg/ml (198.98mM)	Taking the 1 mL working solution as an example, add 94 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	saline	94.000mg/ml (198.98mM)	Taking the 1 mL working solution as an example, add 94 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	saline	94.000mg/ml (198.98mM)	Taking the 1 mL working solution as an example, add 94 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Clear solution	PBS Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	15.000mg/ml (31.75mM)	Taking the 1 mL working solution as an example, add 15 mg of this product to 1 ml of PBS, mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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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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