1. Epigenetics
  2. Histone Demethylase
  3. T-448

T-448 

Cat. No.: HY-122635A Purity: 98.86%
Handling Instructions

T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons.

For research use only. We do not sell to patients.

T-448 Chemical Structure

T-448 Chemical Structure

CAS No. : 1597426-53-3

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 833 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

T-448 is a specific, orally active and irreversible inhibitor of lysine-specific demethylase 1 (LSD1, an H3K4 demethylase), with an IC50 of 22 nM. T-448 enhances H3K4 methylation in primary cultured rat neurons[1].

IC50 & Target

IC50: 22 nM (LSD1)[1].

In Vitro

T-448 enhances the levels of H3K4 methylation, increased mRNA expression of neural plasticity-related genes including brain derived neurotrophic factor (Bdnf), and ameliorated learning dysfunction[1].

RT-PCR[1].

Cell Line: Primary cultured rat neurons.
Concentration: 0-10 μM.
Incubation Time: 1 day treatment.
Result: Increased Ucp2 H3K4me2 and Ucp2 mRNA significantly.
In Vivo

T-448 has minimal impact on the LSD1-GFI1B complex and a superior hematological safety profile in mice via the generation of a compact formyl-FAD adduct. T-448 increases brain H3K4 methylation and partially restored learning function in mice with NMDA receptor hypofunction[1].
T-448 increases H3K4 methylation in the brain without causing hematological side effects even at 100 mg/kg[1].

Animal Model: NR1-hypo mice[1].
Dosage: 1, 10 mg/kg.
Administration: Orally, 3 weeks.
Result: Dose-dependently increased the H3K4me2 levels around Bdnf, Arc, and Fos genes in the mouse hippocampus.
Resulted in partial but statistically significant and dosedependent rescue effects on the rate of correct choices in NR1-hypo mice.
Molecular Weight

386.50

Formula

C₁₇H₂₀N₄OS.₁/₂C₄H₄O₄

CAS No.

1597426-53-3

SMILES

O=C(NC1=NN=C(C)S1)C2=CC=CC([[email protected]]3[[email protected]](NC4CCC4)C3)=C2.O=C(O)/C=C/C(O)=O.[1/2]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (43.13 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5873 mL 12.9366 mL 25.8732 mL
5 mM 0.5175 mL 2.5873 mL 5.1746 mL
10 mM 0.2587 mL 1.2937 mL 2.5873 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (4.32 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.86%

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Keywords:

T-448T448T 448Histone DemethylaseInhibitorinhibitorinhibit

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T-448
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HY-122635A
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