2. PROTAC Cell Cycle/DNA Damage Immunology/Inflammation
  3. Molecular Glues NEKs Interleukin Related
  4. LC-04-045

LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia.

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LC-04-045

LC-04-045 構造式

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1220 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1220 在庫あり
Solid
1 mg $490 在庫あり
5 mg $980 在庫あり
10 mg $1320 在庫あり
25 mg $2180 在庫あり
50 mg $2950 在庫あり
100 mg $3980 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

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Based on 0 publication(s) in Google Scholar

LC-04-045 関連抗体

Top Publications Citing Use of Products

NEKs 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
NEK1 NEK2 NEK4 NEK6 NEK7

Interleukin Related 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
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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  • 純度とドキュメンテーション

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製品説明

LC-04-045 is a selective NIMA-related kinase 7 (NEK7) molecular glue degrader. LC-04-045 induces NEK7 degradation via the CRBN-based ubiquitin-proteasome system, dependent on the glycine 57-containing degron motif. LC-04-045 inhibits secretion of downstream cytokines IL-1β and IL-18. LC-04-045 can be used for the research of lymphoblastic leukemia[1].

IC50 & Target[1]

NEK7

7 nM (DC50)

IL-1β

 

IL-18

 

体外実験

LC-04-045 (0.007 μM; 6 h) potently degrades NEK7 in MOLT-4 cells with a DC50 of 7 nM and a Dmax of 90%[1].
LC-04-045 (37 nM-10 μM; 0-24 h) induces time-dependent NEK7 degradation in MOLT-4 cells[1].

LC-04-045 promotes formation of a CRBN:MGD:NEK7 ternary complex in HEK293T cells with an EC50 of 33 nM[1].
LC-04-045 (6 h) selectively degrades wildtype NEK7, but not NEK7 variants with G57N, R35A, or R50A mutations, in MOLT-4 cells after 6 h of treatment, confirming dependence on the G57-containing degron motif and adjacent R35/R50 residues for activity[1].
LC-04-045 (37 nM-10 μM; 24 h) potently degrades NEK7 in PBMCs with a DC50 of 2.9 nM and a Dmax of 90% after 24 h of treatment[1].
LC-04-045 (1.5 nM-10 μM; 16 h) potently degrades NEK7 in LPS (HY-D1056)-stimulated hMDMs with a DC50 of 40 nM and a Dmax of 88%[1].
LC-04-045 (0.01 nM-10000 nM) effectively inhibits LPS-stimulated secretion of IL-1β (IC50 = 33.03 nM) and IL-18 (IC50 = 32.99 nM) in hMDMs[1].

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

LC-04-045 関連抗体

Western Blot Analysis[1]

Cell Line: MOLT-4
Concentration: 37, 111, 333 nM, 1, 10 μM
Incubation Time: 6 h
Result: Induced time-dependent NEK7 degradation.
Did not affect protein levels of NEK1, NEK2, NEK4, NEK10, or NEK11.
分子量

566.05

分子式

C32H28ClN5O3
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H](N(CC1=C2C=CC(C3=CN=C4CN(CC5=CC=CC=C5C6=CC=CC=C6Cl)CCN43)=C1)C2=O)CC7)NC7=O
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 : 100 mg/mL (176.66 mM; Need ultrasonic; 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 1.7666 mL 8.8331 mL 17.6663 mL
5 mM 0.3533 mL 1.7666 mL 3.5333 mL
10 mM 0.1767 mL 0.8833 mL 1.7666 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
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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: ≥ 5 mg/mL (8.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (8.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 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.
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, 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 1.7666 mL 8.8331 mL 17.6663 mL 44.1657 mL
5 mM 0.3533 mL 1.7666 mL 3.5333 mL 8.8331 mL
10 mM 0.1767 mL 0.8833 mL 1.7666 mL 4.4166 mL
15 mM 0.1178 mL 0.5889 mL 1.1778 mL 2.9444 mL
20 mM 0.0883 mL 0.4417 mL 0.8833 mL 2.2083 mL
25 mM 0.0707 mL 0.3533 mL 0.7067 mL 1.7666 mL
30 mM 0.0589 mL 0.2944 mL 0.5889 mL 1.4722 mL
40 mM 0.0442 mL 0.2208 mL 0.4417 mL 1.1041 mL
50 mM 0.0353 mL 0.1767 mL 0.3533 mL 0.8833 mL
60 mM 0.0294 mL 0.1472 mL 0.2944 mL 0.7361 mL
80 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5521 mL
100 mM 0.0177 mL 0.0883 mL 0.1767 mL 0.4417 mL
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LC-04-045 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:

LC-04-045Molecular GluesNEKsInterleukin RelatedNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesILlymphoblastic leukemia cellsNEK7HEK293T cellsinflammatory diseasesIL-1βIL-18ubiquitin-proteasome systemMOLT-4 cellsCRBNglycine 57-containing degron motifInhibitorinhibitorinhibit

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製品名:
LC-04-045
製品番号:
HY-172162
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