2. Epigenetics
  3. Histone Demethylase
  4. KDM5B-IN-4

KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs.

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KDM5B-IN-4 Chemical Structure

KDM5B-IN-4 Chemical Structure

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Based on 1 publication(s) in Google Scholar

KDM5B-IN-4 Related Antibodies

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Description

KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs[1].

IC50 & Target

IC 50: 0.025 μM (Lysine demethylase 5B, KDM5B)[1].
In Vitro

KDM5B-IN-4 (20 μM, 72 h) has targeted inhibition of KDM5B and induction of H3K4me1/2/3 production in PC-3 cells[1].
KDM5B-IN-4 (0-20 μM; 72 h) not only targets KDM5B in cells, but also induces H3K4me1/2/3 accumulation in PC-3 cells[1].
KDM5B-IN-4 (0-10 μM, 0-24 h) inhibited the proliferation and migration of prostate cancer cells, blocked the PC-3 cycle in the G2/M phase, and induced apoptosis of PC-3 cells to a certain extent[1].

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

KDM5B-IN-4 Related Antibodies

Western Blot Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10, 20 μM
Incubation Time: 72 h
Result: Induced the concentrations of H3K4me1/2/3 significantly different from those of the control, and the results obtained were similar to those obtained using the CPI-455 positive control.
Had no significant effect on P110α, P85, and pAKT at low concentration levels (0-10μM), and P110α, P85, and pAKT were significantly decreased when 11ad was at high concentration (20 μM).

Cell Migration Assay [1]

Cell Line: PC-3
Concentration: 0, 5, 10 μM
Incubation Time: 0, 6, 12, 24 h
Result: Inhibited colony formation in a dosedependent manner, especially at high doses (10 μM).

Cell Cycle Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Blocked the cell cycle at G2/M phase in 10 μM.

Apoptosis Analysis[1]

Cell Line: PC-3
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced PC-3 cell apoptosis in a dose-dependent manner (7.58%, 26.14%, 28.20%, 45.66%).
In Vivo

KDM5B-IN-4 (50 mg/kg, i.g., 50 mg/kg/d, 13 days) treatment at 50 mg/kg was slightly better than the efficacy of DOX[1].
KDM5B-IN-4 (50 mg/kg, i.g., 50 mg/kg/d, 25 days) did not cause noticeable damage to the mice, confirming that 11ad had no significant toxicity or side effects in vivo[1].
Pharmacokinetic Analysis in KDM5B-IN-4 (compound 11ad) Xenograft Model[1]

KDM5B-IN-4 (compound 11ad) 药代动力学分析[1]

Parameter T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (h*ng/mL) MRT0-t (h) Vz (L/kg) Cl (L•h/kg) F
p.o. (25mg/kg) 5.30 6.0 411.67 3024.33 6.90 / / 20.28%
i.v. (5mg/kg) 2.95 0.083 551.67 44437.67 10.29 19.51 0.49 /

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

Animal Model: PC-3 xenograft model in male Spraguee-Dawley rats[1].
Dosage: 25, 50 mg/kg
Administration: Intragastric administration to mice (i.g.) for 25 days, administered once daily.
Result: Compared with NaCl treatment, treatment with 25 mg/kg and 50 mg/kg significantly decreased tumor volume.
Animal Model: PC-3 xenograft model in male Spraguee-Dawley rats[1].
Dosage: 2 g/kg
Administration: Intragastric administration to mice (i.g.) for 14 days, administered once daily.
Result: No significant loss of major organs in the high-dose and low-dose groups.
Molecular Weight

490.60

Formula

C30H30N6O
Appearance

Solid

Color

White to off-white

SMILES

CN1CCN(CC1)CCNC(C2=CC(C3=CC=C4C=CC=CC4=C3)=NC5=C2C=NN5C6=CC=CC=C6)=O
Shipping

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

DMSO : 33.33 mg/mL (67.94 mM; ultrasonic and adjust pH to 2 with 1 M HCL; 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 2.0383 mL 10.1916 mL 20.3832 mL
5 mM 0.4077 mL 2.0383 mL 4.0766 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
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Concentration
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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: ≥ 3.33 mg/mL (6.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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: ≥ 3.33 mg/mL (6.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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

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 2.0383 mL 10.1916 mL 20.3832 mL 50.9580 mL
5 mM 0.4077 mL 2.0383 mL 4.0766 mL 10.1916 mL
10 mM 0.2038 mL 1.0192 mL 2.0383 mL 5.0958 mL
15 mM 0.1359 mL 0.6794 mL 1.3589 mL 3.3972 mL
20 mM 0.1019 mL 0.5096 mL 1.0192 mL 2.5479 mL
25 mM 0.0815 mL 0.4077 mL 0.8153 mL 2.0383 mL
30 mM 0.0679 mL 0.3397 mL 0.6794 mL 1.6986 mL
40 mM 0.0510 mL 0.2548 mL 0.5096 mL 1.2740 mL
50 mM 0.0408 mL 0.2038 mL 0.4077 mL 1.0192 mL
60 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8493 mL
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KDM5B-IN-4 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:

KDM5B-IN-4Histone DemethylasePC-3LNCaPhuman prostate cancer cellPC-3 xenograft modelprostate cancer.Inhibitorinhibitorinhibit

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