2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC Histone Demethylase
  4. 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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LSD1/HDAC-IN-3

LSD1/HDAC-IN-3 Chemical Structure

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LSD1/HDAC-IN-3 Related Antibodies

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Description

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)[1].

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.

LSD1/HDAC-IN-3 Related Antibodies
In Vivo

LSD1/HDAC-IN-3 (Compound (±)-3d) (10 μM (1 μL/eye), intravitreal injection, single bilateral administration) enhances photoreceptor survival in retinal tissues of rd10 mice with homozygous Pde6b mutation on C57Bl/6J background[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 10 μM (1 μL/eye)
Administration: intravitreal injection, single bilateral administration
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.
Molecular Weight

440.58

Formula

C28H32N4O
SMILES

O=C(NC1=CC=CC=C1N)C(C=C2)=CC=C2CN(CC3)CCC3N[C@H](C4)[C@@H]4C5=CC=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LSD1/HDAC-IN-3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LSD1/HDAC-IN-3HDACHistone DemethylaseHistone deacetylasesLSD1retinitis pigmentosaARPE-19661W retinal cellsInhibitorinhibitorinhibit

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