2. Epigenetics
  3. Histone Demethylase
  4. GSK467

GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.

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GSK467

GSK467 構造式

CAS 番号 : 1628332-52-4

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 203 在庫あり
Solution
10 mM * 1 mL in DMSO USD 203 在庫あり
Solid
5 mg $185 在庫あり
10 mg $278 在庫あり
25 mg $500 在庫あり
50 mg $800 在庫あり
100 mg $1100 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 5 publication(s) in Google Scholar

GSK467 関連抗体

Top Publications Citing Use of Products

Histone Demethylase アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members[1][2].

IC50 & TargetHY-116761 [1]

KDM5

10 nM (Ki)

KDM5

26 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
U2OS IC50
2 μM
Compound: 41
Inhibition of N-terminal his-tagged full-length human KDM4C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs
Inhibition of N-terminal his-tagged full-length human KDM4C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs
[PMID: 26771203]
U2OS IC50
2.5 μM
Compound: 41
Inhibition of human KDM5C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs
Inhibition of human KDM5C transfected in U2OS cells assessed as inhibition of H3K9Me3 demethylation for 24 hrs
[PMID: 26771203]
体外実験

GSK467 (0-100 μM; 6 days) shows antiproliferative effect against human multiple myeloma tumor cells[1].
? GSK467 is located in the 2-OG-binding pocket[2].
? GSK467 inhibits spheroid formation, colony formation, invasion and migration of HCC cells[3].

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

GSK467 関連抗体

Cell Proliferation Assay[1]

Cell Line: Human multiple myeloma tumor cell line MM.1S
Concentration: 0-100 μM
Incubation Time: 6 days
Result: Showed antiproliferative effect with an IC50 of >50 μM.
体内実験

GSK-467 can inhibit the proliferation and growth of HCC tumor cells by promoting the expression of miR-448 and inhibiting the YTHDF3/ITGA6 pathway in female BALB/c nude mice[3].

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

319.32

分子式

C17H13N5O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(NC(OC3=CN(N=C3)CC4=CC=CC=C4)=N1)C=NC=C2
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 20.83 mg/mL (65.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1317 mL 15.6583 mL 31.3165 mL
5 mM 0.6263 mL 3.1317 mL 6.2633 mL
10 mM 0.3132 mL 1.5658 mL 3.1317 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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 (6.51 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (6.51 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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:  15% Cremophor EL    85% Saline

    Solubility: 5 mg/mL (15.66 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  1% CMC-Na/saline water

    Solubility: 2.5 mg/mL (7.83 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.
純度とドキュメンテーション
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1317 mL 15.6583 mL 31.3165 mL 78.2914 mL
5 mM 0.6263 mL 3.1317 mL 6.2633 mL 15.6583 mL
10 mM 0.3132 mL 1.5658 mL 3.1317 mL 7.8291 mL
15 mM 0.2088 mL 1.0439 mL 2.0878 mL 5.2194 mL
20 mM 0.1566 mL 0.7829 mL 1.5658 mL 3.9146 mL
25 mM 0.1253 mL 0.6263 mL 1.2527 mL 3.1317 mL
30 mM 0.1044 mL 0.5219 mL 1.0439 mL 2.6097 mL
40 mM 0.0783 mL 0.3915 mL 0.7829 mL 1.9573 mL
50 mM 0.0626 mL 0.3132 mL 0.6263 mL 1.5658 mL
60 mM 0.0522 mL 0.2610 mL 0.5219 mL 1.3049 mL
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GSK467 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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:

GSK4671628332-52-4GSK 467GSK-467Histone Demethylasehuman multiple myeloma tumoranticancerJARID1BPLU1HCCInhibitorinhibitorinhibit

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製品名:
GSK467
製品番号:
HY-116761
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