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1062368-62-0 (LDN193189 (Hydrochloride))

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Identification

LDN193189 (Hydrochloride) LDN193189 (Hydrochloride)
Name LDN193189 (Hydrochloride)
Formula C25H26Cl4N6
MW 552.33
CAS No. 1062368-62-0
EINECS
Smiles [H]Cl.[H]Cl.[H]Cl.[H]Cl.C1(C2=C3N=CC(C4=CC=C(N5CCNCC5)C=C4)=CN3N=C2)=CC=NC6=CC=CC=C16
Synonyms LDN 193189 hydrochloride; LDN-193189 hydrochloride; 4-(6-(4-(piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline tetrahydrochloride
InChI InChI=1S/C25H22N6.4ClH/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30;;;;/h1-10,15-17,26H,11-14H2;4*1H
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Introduction

LDN193189 4Hcl(DM 3189) is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. IC50 value: 5 nM/30 nM (ALK2/ALK3) [1] Target: ALK2/3 in vitro: LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively.

Background Information

LDN193189 4Hcl(DM 3189) is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β. IC50 value: 5 nM/30 nM (ALK2/ALK3) [1] Target: ALK2/3 in vitro: LDN193189 potently inhibits BMP4-mediated Smad1, Smad5 and Smad8 activation with IC50 of 5 nM, and efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively. Furthermore, LDN193189 also shows the inhibitory effect on the transcriptional activity induced by either constitutively active ALK2R206H or ALK2Q207D mutant proteins [1]. A recent study shows that LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells [4]. in vivo: In conditional caALK2-transgenic mice with Ad.Cre on on postnatal day 7 (P7), LDN-193189 (3 mg/kg i.p) leads to mild calcifications surrounding the left tibia and fibula first visible at P13, and prevents radiographic lesions at P15 without causing weight loss or growth retardation, spontaneous fractures, decreased bone density or behavioral abnormalities [1]. LDN193189 dorsalizes zebrafish embryos by inhibiting signaling pathways induced by bone morphogenetic protein (BMP)6 without effect on vascular development [2]. In PCa-118b tumor-bearing mice, LDN-193189 treatment attenuates tumor growth and reduces bone formation in the tumors [3]. In LDL receptor-deficient (LDLR-/-) mice, LDN-193189 potently inhibits development of atheroma. Moreover, LDN-193189 also exhibits the inhibitory effects on associated vascular inflammation, osteogenic activity, and calcification [4]. ......by MedChemexpress Co., Ltd.
LDN193189 HCl is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, 200-fold selectivity for BMP versus TGF-β. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:Light yellow to yellow solid EBNumber:EB000019279

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways TGF-beta/Smad
Target TGF-β Receptor
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
LDN193189 (Hydrochloride) - Not Found
LDN193189 (Hydrochloride) - No Development Reported
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Safety Data of LDN193189 (Hydrochloride)

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
AbMole BioScience 5mg/USD130(In stock) USA
Apexbio Technology LLC 5mg/USD85(In stock);10mg/USD160(In stock) USA
CHEMSCENE, LLC 5mg/USD70(In stock);10mg/USD90(In stock);50mg/USD240(In stock) USA
EMD Millipore 10mg/USD189() USA
MedChemexpress Co., Ltd. 5mg/USD70(In stock);10mg/USD90(In stock);50mg/USD240(In stock) USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD86(In stock);10mg/USD160(In stock);50mg/USD602(In stock) China
Target Molecule Corp. 2mg/USD49();5mg/USD82();10mg/USD128();25mg/USD198();50mg/USD318() USA
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Related Products

Other Forms of 1062368-62-0

Name CAS No Formula MW
LDN193189 1062368-24-4 C25H22N6 406.48

Recommended Compounds in TGF-β Receptor

Name CAS No Formula MW
K 02288 1431985-92-0 C20H20N2O4 352.38
ML347 1062368-49-3 C22H16N4O 352.39
DMH-1 1206711-16-1 C24H20N4O 380.44
LDN-212854 1432597-26-6 C25H22N6 406.48
SB-505124 (hydrochloride) 356559-13-2 C20H22ClN3O2 371.86
A 77-01 607737-87-1 C18H14N4 286.33
SB-505124 694433-59-5 C20H21N3O2 335.4
LY-364947 396129-53-6 C17H12N4 272.3
SD-208 627536-09-8 C17H10ClFN6 352.75
RepSox 446859-33-2 C17H13N5 287.32
LDN193189 1062368-24-4 C25H22N6 406.48
A 83-01 909910-43-6 C25H19N5S 421.52
LY2109761 700874-71-1 C26H27N5O2 441.52
LY2157299 700874-72-2 C22H19N5O 369.42
GW788388 452342-67-5 C25H23N5O2 425.48
SB 525334 356559-20-1 C21H21N5 343.42
SB-431542 301836-41-9 C22H16N4O3 384.39
EW-7197 1352608-82-2 C22H18FN7 399.42
R-268712 879487-87-3 C20H18FN5O 363.39
ITD-1 1099644-42-4 C27H29NO3 415.52

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

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References

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More Information

LDN193189 (Hydrochloride)

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