2. Epigenetics Apoptosis
  3. Histone Demethylase Apoptosis
  4. SKLB325

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .

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SKLB325 Chemical Structure

SKLB325 Chemical Structure

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 520 In-stock
25 mg USD 980 In-stock
50 mg USD 1420 In-stock
100 mg USD 1950 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

SKLB325 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

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis[1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2].

In Vitro

SKLB325 suppresses ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth[1].
SKLB325 (0.25-16 μM; for 24-72 h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4 μM, and the optimal duration of action is 72 h[1].
SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro[1].

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

SKLB325 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: SKOV3, ES2, A2780s and CP70 cells
Concentration: 0, 0.25, 0.5, 1, 2, 4, 8, and 16 μM
Incubation Time: 24 h, 48 h, and 72 h
Result: With increasing SKLB325 concentration, the inhibitory effect also increased, exhibiting a significant dose-response relationship. There was a significant difference between the drug group across different doses and the control group.

Western Blot Analysis[1]

Cell Line: SKOV3, ES2 and A2780s cells
Concentration: 4 μM
Incubation Time: 72 hours
Result: p53, p21, and PUMA protein levels were significantly upregulated in SKOV3, ES2 and A2780s cells.
In Vivo

SKLB325 (10 mg/kg) has antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice[1].

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

Animal Model: Female athymic BALB/c nude mice[1]
Dosage: 10 mg/kg
Administration: I.p. injections every three days for eight doses total
Result: The average weight of intraperitoneal tumor nodules was 1.56 ± 0.70, 1.04 ± 0.62, and 0.14 ± 0.11 g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.
Molecular Weight

244.25

Formula

C12H12N4O2
Appearance

Solid

Color

White to off-white

SMILES

OC1=NC(N/N=C/C2=CC=CC=C2O)=NC(C)=C1
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 : 20.83 mg/mL (85.28 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 4.0942 mL 20.4708 mL 40.9417 mL
5 mM 0.8188 mL 4.0942 mL 8.1883 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)

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Concentration
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Volume
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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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Volume (start)

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C2

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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 (8.52 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:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 4.0942 mL 20.4708 mL 40.9417 mL 102.3541 mL
5 mM 0.8188 mL 4.0942 mL 8.1883 mL 20.4708 mL
10 mM 0.4094 mL 2.0471 mL 4.0942 mL 10.2354 mL
15 mM 0.2729 mL 1.3647 mL 2.7294 mL 6.8236 mL
20 mM 0.2047 mL 1.0235 mL 2.0471 mL 5.1177 mL
25 mM 0.1638 mL 0.8188 mL 1.6377 mL 4.0942 mL
30 mM 0.1365 mL 0.6824 mL 1.3647 mL 3.4118 mL
40 mM 0.1024 mL 0.5118 mL 1.0235 mL 2.5589 mL
50 mM 0.0819 mL 0.4094 mL 0.8188 mL 2.0471 mL
60 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7059 mL
80 mM 0.0512 mL 0.2559 mL 0.5118 mL 1.2794 mL
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SKLB325 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:

SKLB325SKLB 325SKLB-325Histone DemethylaseApoptosisGynaecologicalcancerJMJD6ovarianrenalcarcinomaRCCInhibitorinhibitorinhibit

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