2. Cell Cycle/DNA Damage Apoptosis
  3. DNA/RNA Synthesis Apoptosis
  4. YL-5092

YL-5092 is a selective YT521-B homology (YTH) domain-containing protein 1 (YTHDC1) inhibitor with an IC50 of 7.4 nM and a KD of 29.6 nM. YL-5092 can suppress cancer cell proliferation and induce cell G0/G1 phase arrest and apoptosis. YL-5092 can be used for the research of cancer, such as acute myeloid leukemia (AML).

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YL-5092

YL-5092 構造式

CAS 番号 : 3056857-07-6

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 269 在庫あり
Solution
10 mM * 1 mL in DMSO USD 269 在庫あり
Solid
5 mg $245 在庫あり
10 mg $390 在庫あり
25 mg $780 在庫あり
50 mg $1250 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

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YL-5092 関連抗体

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DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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製品説明

YL-5092 is a selective YT521-B homology (YTH) domain-containing protein 1 (YTHDC1) inhibitor with an IC50 of 7.4 nM and a KD of 29.6 nM. YL-5092 can suppress cancer cell proliferation and induce cell G0/G1 phase arrest and apoptosis. YL-5092 can be used for the research of cancer, such as acute myeloid leukemia (AML)[1].

IC50 & Target[1]

YTHDC1

7.4 nM (IC50)

YTHDC1

29.6 nM (Kd)

体外実験

YL-5092 inhibits acute myeloid leukemia cell with IC50 values of 0.28-2.87 μM[1].
YL-5092 (0.1-30 μM, 6 h) stabilizes YTHDC1 in MOLM-13 and U937 cells[1].
YL-5092 (1 μM) blocks the binding of YTHDC1 with its substrates (m6A-mRNAs) in HEK293T cells[1].
YL-5092 (1 μM) reduces MYC mRNA levels in MOLM-13 cells[1].
YL-5092 (0.25-2 μM, 48-120 h) induces G0/G1 phase arrest and increases apoptotic cells in MOLM-13 cells[1].
YL-5092 (1-3 μM, 14-16 days) inhibits the colony-forming ability of CD34+ cells[1].

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

YL-5092 関連抗体

Cell Cycle Analysis[1]

Cell Line: MOLM-13 cells
Concentration: 0.25, 0.5, 1 and 2 μM
Incubation Time: 48 h
Result: Increased cells in G0/G1 phase.
体内実験

YL-5092 (70 mg/kg, i.p., twice a day for 18 days) impairs leukemogenesis and improves the animal survival rate in mouse MOLM-13/U937 tumor xenograft models[1].

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

Animal Model: Mouse MOLM-13/U937 tumor xenograft models[1]
Dosage: 70 mg/kg
Administration: Intraperitoneally injection, twice a day for 18 days
Result: Alleviated the development of leukemia and significantly prolonged the survival rate of mice.
Reduced leukemia infiltration in the peripheral blood, spleen, and bone marrow.
Reduced the expression of YTHDC1 target genes, including MYC, FOXM1, GINS1, MCM2, MCM4 and MCM5.
Had no weight loss.
分子量

441.43

分子式

C22H14F3N3O2S
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CNC(C(NC2=CC=C(C3=CN=CS3)C=C2)=O)=C1)C4=C(C(F)(F)F)C=CC=C4
輸送条件

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

DMSO : 100 mg/mL (226.54 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 2.2654 mL 11.3268 mL 22.6536 mL
5 mM 0.4531 mL 2.2654 mL 4.5307 mL
10 mM 0.2265 mL 1.1327 mL 2.2654 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
×
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: ≥ 2.5 mg/mL (5.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 2.2654 mL 11.3268 mL 22.6536 mL 56.6341 mL
5 mM 0.4531 mL 2.2654 mL 4.5307 mL 11.3268 mL
10 mM 0.2265 mL 1.1327 mL 2.2654 mL 5.6634 mL
15 mM 0.1510 mL 0.7551 mL 1.5102 mL 3.7756 mL
20 mM 0.1133 mL 0.5663 mL 1.1327 mL 2.8317 mL
25 mM 0.0906 mL 0.4531 mL 0.9061 mL 2.2654 mL
30 mM 0.0755 mL 0.3776 mL 0.7551 mL 1.8878 mL
40 mM 0.0566 mL 0.2832 mL 0.5663 mL 1.4159 mL
50 mM 0.0453 mL 0.2265 mL 0.4531 mL 1.1327 mL
60 mM 0.0378 mL 0.1888 mL 0.3776 mL 0.9439 mL
80 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7079 mL
100 mM 0.0227 mL 0.1133 mL 0.2265 mL 0.5663 mL
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YL-5092 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:

YL-50923056857-07-6YL5092YL 5092DNA/RNA SynthesisApoptosisYTHYTHDC1AMLMOLM-13U937Inhibitorinhibitorinhibit

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製品名:
YL-5092
製品番号:
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