2. Epigenetics
  3. Histone Demethylase
  4. Seclidemstat

Seclidemstat (SP-2577) est un inhibiteur de LSD1 qui est puissant et oralement biodisponible, avec un IC50 moyen de 127 nM.

Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.

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

Seclidemstat Chemical Structure

Seclidemstat Chemical Structure

CAS No. : 1423715-37-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Seclidemstat:

Seclidemstat 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

Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma[1][2].

IC50 & Target

KDM1/LSD1

 

In Vitro

Seclidemstat (72 hours) inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells)[2].
? Seclidemstat (72 hours) promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells)[2].
? Seclidemstat (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line[2].

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

Seclidemstat Related Antibodies
Clinical Trial
Molecular Weight

450.94

Formula

C20H23ClN4O4S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(N/N=C(C1=CC(Cl)=CC=C1O)\C)C2=CC=CC(S(=O)(N3CCN(C)CC3)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (110.88 mM; ultrasonic and warming and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2176 mL 11.0879 mL 22.1759 mL
5 mM 0.4435 mL 2.2176 mL 4.4352 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  1.6% DMA    5% Ethanol    45% PEG400    48.4% PBS

    Solubility: 2 mg/mL (4.44 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (22.18 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.77%

SDS (393 KB)

COA (246 KB) HNMR (261 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2176 mL 11.0879 mL 22.1759 mL 55.4397 mL
5 mM 0.4435 mL 2.2176 mL 4.4352 mL 11.0879 mL
10 mM 0.2218 mL 1.1088 mL 2.2176 mL 5.5440 mL
15 mM 0.1478 mL 0.7392 mL 1.4784 mL 3.6960 mL
20 mM 0.1109 mL 0.5544 mL 1.1088 mL 2.7720 mL
25 mM 0.0887 mL 0.4435 mL 0.8870 mL 2.2176 mL
30 mM 0.0739 mL 0.3696 mL 0.7392 mL 1.8480 mL
40 mM 0.0554 mL 0.2772 mL 0.5544 mL 1.3860 mL
50 mM 0.0444 mL 0.2218 mL 0.4435 mL 1.1088 mL
60 mM 0.0370 mL 0.1848 mL 0.3696 mL 0.9240 mL
80 mM 0.0277 mL 0.1386 mL 0.2772 mL 0.6930 mL
100 mM 0.0222 mL 0.1109 mL 0.2218 mL 0.5544 mL
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Seclidemstat Related Classifications

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:

Seclidemstat1423715-37-0SP-2577SP2577SP 2577Histone DemethylasereversibleantitumorimmunitySWI/SNFcomplexDNAreplicationEwingSarcomaInhibitorinhibitorinhibit

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