2. Epigenetics Immunology/Inflammation Apoptosis
  3. Histone Demethylase CD44 Apoptosis
  4. LSD1-IN-48

LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia.

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

LSD1-IN-48

LSD1-IN-48 Chemical Structure

CAS No. : 3104325-26-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

LSD1-IN-48 Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

View All Isoforms
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

LSD1-IN-48 is a tranylcypromine-pyrimidine derivative and selective LSD1 inhibitor with a human IC50 of 7.87 nM. LSD1-IN-48 increases H3K4me1/2 histone methylation levels. LSD1-IN-48 induces apoptosis, upregulates CD86, downregulates SOX2 and CD44, inhibits proliferation in cancer cells. LSD1-IN-48 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

LSD1

7.87 nM (IC50)

In Vitro

LSD1-IN-48 (7a) potently inhibits recombinant LSD1 with an IC50 of 7.87 nM and exhibits over 127-fold and 1270-fold selectivity for LSD1 over MAO-A and MAO-B, respectively[1].
LSD1-IN-48 inhibits the proliferation of MV-4-11, HL-60, and THP-1 acute myeloid leukemia cells with IC50 values of 0.36 μM, 0.48 μM, and 1.12 μM, respectively[1].
LSD1-IN-48 (10-100 μM) directly binds to LSD1 extracted from MV-4-11 cells, protecting the protein from alkaline protease hydrolysis in a dose-dependent manner[1].
LSD1-IN-48 shows metabolic stability in human liver microsomes with a half-life of 7.26 min and an intrinsic clearance of 172 mL/min/kg[1].
LSD1-IN-48 (0.5-2 μM; 2 days) increases H3K4me1 and H3K4me2 histone methylation levels in MV-4-11 cells in a dose-dependent manner[1].
LSD1-IN-48 (0.5-2 μM; 2 days) induces apoptosis in MV-4-11 cells in a dose-dependent manner and activates the caspase-mediated apoptotic pathway[1].
LSD1-IN-48 (0.5-2 μM; 4 days) dose-dependently upregulates the differentiation marker CD86 in MV-4-11 cells[1].
LSD1-IN-48 (0.5-2 μM; 96 h) dose-dependently reduces the levels of stem cell-associated proteins SOX2 and CD44 in MV-4-11 cells,[1].

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

LSD1-IN-48 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 2 days
Result: Dose-dependently increased the levels of H3K4me1 and H3K4me2; at 2 μM, H3K4me1 levels increased to ~4-fold and H3K4me2 levels increased to ~1.5-fold relative to the control.

Apoptosis Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 2 days
Result: Dose-dependently increased the total apoptosis rate; at 2 μM, the total apoptosis rate increased from 6.45% to 33.19%.
Dose-dependently increased the levels of cleaved caspase-3, cleaved caspase-7, and cleaved PARP.

Cell Differentiation Assay[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 4 days
Result: Dose-dependently increased CD86 expression; at 2 μM, CD86 expression increased by 19.18% relative to the control.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 96 h
Result: Dose-dependently reduced the protein levels of SOX2 and CD44; at 2 μM, SOX2 levels were reduced to ~0.15-fold and CD44 levels were reduced to ~0.55-fold relative to the control.
Parmacokinetics
Species Dose Route AUC0-∞ AUC0-t T1/2 Cmax CL
Rat[1] 1 mg/kg i.v. 26.0 μg/L·h 22.9 μg/L·h 0.863 h 57.2 μg/L 38794 mL/h/kg
Molecular Weight

436.44

Formula

C18H18F2N6O3S
CAS No.
SMILES

O=S(C1=NC(N2C=C(CN[C@@H]3C[C@H]3C4=CC=C(F)C=C4F)N=N2)=CC(OC)=N1)(C)=O
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

LSD1-IN-48 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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-IN-483104325-26-7Histone DemethylaseCD44ApoptosisIn (Lu)-related protein p80Pgp-1/Ly-24ECMRIIIHUTCH-1H3K4me2CD86apoptosisH3K4me1LSD1MAO-Aacute myeloid leukemiaMAO-BSOX2Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LSD1-IN-48
Cat. No.:
HY-181781
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.