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LDN-193189 dihydrochloride

Cat. No. M2805
LDN-193189 dihydrochloride Structure
Synonym:

DM-3189 dihydrochloride

Size Price Availability Quantity
2mg USD 50  USD50 In stock
5mg USD 78  USD78 In stock
10mg USD 110  USD110 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

LDN-193189 dihydrochloride 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. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva. LDN-193189 targets GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors. LDN-193189 (0.05, 0.5, 5 μM) efficiently inhibits GDF8 induced Smad3/4 reporter gene activity.

Chemical Information
Molecular Weight 479.40
Formula C25H24Cl2N6
CAS Number 1435934-00-1
Solubility (25°C) Water 11 mg/mL
DMSO 8 mg/mL (ultrasonic and warming)
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Arjan van Caam, et al. TGFβ1-induced SMAD2/3 and SMAD1/5 phosphorylation are both ALK5-kinase-dependent in primary chondrocytes and mediated by TAK1 kinase activity

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Keywords: LDN-193189 dihydrochloride, DM-3189 dihydrochloride supplier, ALK, inhibitors, activators


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