2. Epigenetics Metabolic Enzyme/Protease Cell Cycle/DNA Damage Apoptosis
  3. Histone Demethylase E1/E2/E3 Enzyme DNA/RNA Synthesis Caspase Apoptosis
  4. WS-384

WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).

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WS-384 Chemical Structure

WS-384 Chemical Structure

CAS No. : 2247544-03-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

WS-384 Related Antibodies

Top Publications Citing Use of Products

View All Histone Demethylase Isoform Specific Products:

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target

IC50: 338.79 nM (LSD1)[1].
IC50: 14.81 nM (DCN1-UBC12 Protein-protein interaction)[1].
In Vitro

WS-384 (1-32 μM; 24-72 h) inhibits the growth of A549 and H1975 cells in a time- and dose-dependent manner, with an IC50 ranging from 2.15 to 6.67 μM, demonstrating anticancer activity[1].
WS-384 (1-8 μM; 48 h) enhances the expression levels of p21 gene and protein in A549 and H1975 cells by inhibiting the neddylation of cullin 1 and reducing the H3K4 demethylation at the CDKN1A promoter, thus inducing cell cycle arrest at the G2/M phase and apoptosis. Additionally, WS-384 (1-8 μM; 48 h) can also cause DNA damage[1].

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

WS-384 Related Antibodies

Apoptosis Analysis[1]

Cell Line: A549, H1975
Concentration: 1 μM, 2 μM, 4 μM, 8 μM (A549);
0.5 μM, 1 μM, 2 μM, 4 μM (H1975)
Incubation Time: 48 h
Result: Increased the apoptosis rate in a concentration-dependent manner, with the apoptosis rate of A549 cells reaching 44.9% at a concentration of 8 μM and the apoptosis rate of H1975 cells reaching 36.42% at a concentration of 4 μM.

Western Blot Analysis[1]

Cell Line: A549, H1975
Concentration: 2 μM, 4 μM, 8 μM (A549);
1 μM, 2 μM, 4 μM (H1975)
Incubation Time: 48 h
Result: Blocked the neddylation of cullin1 and cullin3 but had no effect on the neddylation of other cullin members (cullin2, cullin4A, and cullin5).
Increased the proteins expression of cleaved caspase 3, cleaved caspase 7, cleaved caspase 9, and cleaved PARP.
Decreased the protein expression of p-CDC2, cyclin B1. CDK4 and CDK6.
Increased the protein expression γ-H2AX (a marker protein of DNA damage).
In Vivo

WS-384 (25-50 mg/kg; p.o.; once daily for 36 consecutive days) effectively inhibits the growth of NSCLC tumors in the BALB/c nude mouse xenograft model with low toxicity[1].

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

Animal Model: BALB/c nude mice xenograft model[1].
Dosage: 25 mg/kg; 50 mg/kg;
Administration: Oral gavage (p.o.); Once daily for 36 consecutive days
Result: Significantly reduced tumor weight and volume in mice in the 50 mg/kg group.
Had no significant toxic effects on the heart, liver, spleen, lungs, and kidneys.
Molecular Weight

542.91

Formula

C18H21BrClN9S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

BrC1=CC=C(CSC2=NN3C(SC4=NN=NN4CCN(C)C)=CC(C)=NC3=N2)C=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 17.86 mg/mL (32.90 mM; ultrasonic and warming and heat to 60°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 1.8419 mL 9.2096 mL 18.4193 mL
5 mM 0.3684 mL 1.8419 mL 3.6839 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

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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: ≥ 1.79 mg/mL (3.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 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:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.79 mg/mL (3.30 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.79 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (17.9 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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 (sealed storage, away from moisture). 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 1.8419 mL 9.2096 mL 18.4193 mL 46.0482 mL
5 mM 0.3684 mL 1.8419 mL 3.6839 mL 9.2096 mL
10 mM 0.1842 mL 0.9210 mL 1.8419 mL 4.6048 mL
15 mM 0.1228 mL 0.6140 mL 1.2280 mL 3.0699 mL
20 mM 0.0921 mL 0.4605 mL 0.9210 mL 2.3024 mL
25 mM 0.0737 mL 0.3684 mL 0.7368 mL 1.8419 mL
30 mM 0.0614 mL 0.3070 mL 0.6140 mL 1.5349 mL
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WS-384 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:

WS-3842247544-03-0WS384WS 384Histone DemethylaseE1/E2/E3 EnzymeDNA/RNA SynthesisCaspaseApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasenon-small cell lung cancer (NSCLC)A549H1975apoptosiscell cycle arrestDNA damageInhibitorinhibitorinhibit

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