Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H22N6.ClH |
Molecular Weight | 442.943 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.C1CN(CCN1)C2=CC=C(C=C2)C3=CN4N=CC(=C4N=C3)C5=CC=NC6=CC=CC=C56
InChI
InChIKey=PCCDKTWDGDFRME-UHFFFAOYSA-N
InChI=1S/C25H22N6.ClH/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;1H
DescriptionSources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19029982Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/18621530; http://www.ncbi.nlm.nih.gov/pubmed/?term=21670081
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19029982
Curator's Comment: description was created based on several sources, including:
https://www.ncbi.nlm.nih.gov/pubmed/18621530; http://www.ncbi.nlm.nih.gov/pubmed/?term=21670081
LDN193189 is a cell-permeable, highly potent and selective BMP pathway inhibitor. It prevents Smad1, Smad5, and Smad8 phosphorylation. It is a useful tool compound to modulate stem cell differentiation (for example, neural differentiation of human ESC/iPSC in combination with SB431542). LDN-193189 blocks the production of reactive oxygen species induced by oxidized LDL during atherogenesis in human aortic endothelial cells. It was also used in animal models to treat FOP and ectopic ossification, as well as NSCLC lung cancer.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P36894 Gene ID: 657.0 Gene Symbol: BMPR1A Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/18621530 |
30.0 nM [IC50] | ||
Target ID: Q04771 Gene ID: 90.0 Gene Symbol: ACVR1 Target Organism: Homo sapiens (Human) Sources: http://www.ncbi.nlm.nih.gov/pubmed/18621530 |
5.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
PubMed
Title | Date | PubMed |
---|---|---|
BMP type I receptor inhibition reduces heterotopic [corrected] ossification. | 2008 Dec |
|
Dorsomorphin inhibits BMP signals required for embryogenesis and iron metabolism. | 2008 Jan |
|
BMP9 is a proliferative and survival factor for human hepatocellular carcinoma cells. | 2013 |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=21670081
Curator's Comment: conditional caALK2-transgenic mice with Ad.Cre
3 mg/kg LDN-193189 was used once or twice daily
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=21946668
0.1 uM final concentration in stem cell differentiation conditions
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Systematic Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
393513
Created by
admin on Sat Dec 16 10:54:48 GMT 2023 , Edited by admin on Sat Dec 16 10:54:48 GMT 2023
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
54613581
Created by
admin on Sat Dec 16 10:54:48 GMT 2023 , Edited by admin on Sat Dec 16 10:54:48 GMT 2023
|
PRIMARY | |||
|
PLH51K438W
Created by
admin on Sat Dec 16 10:54:48 GMT 2023 , Edited by admin on Sat Dec 16 10:54:48 GMT 2023
|
PRIMARY | |||
|
1062368-62-0
Created by
admin on Sat Dec 16 10:54:48 GMT 2023 , Edited by admin on Sat Dec 16 10:54:48 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD