LSD1/HDAC-IN-3
LSD1/HDAC-IN-3 is a inhibitor targeting class I HDAC and LSD1 enzymes. LSD1/HDAC-IN-3 inhibits HDAC1, HDAC2, HDAC3, and LSD1 with IC50 values of 1702 nM, 842 nM, 358 nM, and 1074 nM, respectively. LSD1/HDAC-IN-3 exhibits antioxidant effects in H2O2-stressed ARPE-19 and 661W retinal cells, increasing levels of acetylated and methylated histone H3. LSD1/HDAC-IN-3 enhances photoreceptor survival in the rd10 mouse model of retinitis pigmentosa. LSD1/HDAC-IN-3 can be used for the study of inherited retinal diseases such as retinitis pigmentosa (RP).
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- Formule: C28H32N4O
- Masse moléculaire:440.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
IC50 & Target
[1]|
HDAC1 1702 nM (IC50) |
HDAC2 842 nM (IC50) |
HDAC3 358 nM (IC50) |
LSD1 1074 nM (IC50) |
In Vitro
LSD1/HDAC-IN-3 (Compound (±)-3d) exhibits inhibitory activity against class I HDACs and LSD1, with IC50 values of 1702 nM (HDAC1), 842 nM (HDAC2), 358 nM (HDAC3), and 1074 nM (LSD1), while showing no appreciable inhibition against HDAC6, HDAC8, or HDAC10[1].
LSD1/HDAC-IN-3 (10-30 μM, 24 h) significantly protects ARPE-19 and 661W cells from oxidative damage induced by H2O2, as evidenced by increased cell viability[1].
LSD1/HDAC-IN-3 (10 μM, 24 h) partially increases the levels of acetylated histone H3 (ac-H3) and methylated histone H3 (met-H3) in ARPE-19 and 661W cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rd10 mice (autosomal recessive retinitis pigmentosa model with homozygous Pde6b mutation on C57Bl/6J background, both male and female, postnatal day 40)[1]
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Dosage:10 μM (1 μL/eye)
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Administration:intravitreal injection, single bilateral administration
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Result:Enhanced photoreceptor survival.
Preserved retinal pigment epithelium (RPE) barrier integrity, significantly increasing the number of Zonula Occludens-1 (ZO-1) positive intersections.
Downregulated retinal expression of inflammatory genes, specifically reducing the mRNA levels of GFAP, Ccl2, and Ccl12 in retinal tissues, and decreasing GFAP immunoreactivity.
Promoted histone H3 modifications in retinal tissues, inducing an upward trend in the levels of acetylated histone H3 (ac-H3) and methylated histone H3 (met-H3).
Showed no improvement in retinal function.
Exhibited good in vivo safety, with no signs of general distress or ocular tissue side effects.
Chemical Information
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Masse moléculaire 440.58
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Formule C28H32N4O
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SMILES
O=C(NC1=CC=CC=C1N)C(C=C2)=CC=C2CN(CC3)CCC3N[C@H](C4)[C@@H]4C5=CC=CC=C5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LSD1/HDAC-IN-3 Related Classifications
HY-175671 Related Classifications
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