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LDN-57444

Cat. No. M2807
LDN-57444 Structure
Size Price Availability Quantity
5mg USD 65  USD65 In stock
10mg USD 110  USD110 In stock
25mg USD 250  USD250 In stock
50mg USD 380  USD380 In stock
100mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

LDN-57444 is a reversible, competitive proteasome inhibitor for Uch-L1 with IC50 of 0.88 μM, 28-fold selectivity over isoform Uch-L3.

Chemical Information
Molecular Weight 397.64
Formula C17H11Cl3N2O3
CAS Number 668467-91-2
Solubility (25°C) DMSO 11 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Pan Yuan, et al. UCH-L1 inhibitor LDN-57444 hampers mouse oocyte maturation by regulating oxidative stress and mitochondrial function and reducing ERK1/2 expression

[2] Hai-Lian Bi, et al. The deubiquitinase UCHL1 regulates cardiac hypertrophy by stabilizing epidermal growth factor receptor

[3] Hai-Lian Bi, et al. Inhibition of UCHL1 by LDN-57444 attenuates Ang II-Induced atrial fibrillation in mice

[4] Eiji Kobayashi, et al. Inhibition of UCH-L1 Deubiquitinating Activity with Two Forms of LDN-57444 Has Anti-Invasive Effects in Metastatic Carcinoma Cells

[5] Anna Sankiewicz, et al. Development of surface plasmon resonance imaging biosensors for detection of ubiquitin carboxyl-terminal hydrolase L1

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