1. Apoptosis Epigenetics
  2. Apoptosis YTHDF
  3. YTHDF2-IN-1

YTHDF2-IN-1 (Compound CK-75) is a selective YTHDF2 inhibitor (Kd = 26.2 μM). YTHDF2-IN-1 binds to a small hydrophobic pocket on the YTH domain of YTHDF2, disrupting the interaction between YTHDF2 and m6A-modified RNA. YTHDF2-IN-1 induces cell cycle arrest and Apoptosis. YTHDF2-IN-1 is applicable to research on chronic myeloid leukemia, colon cancer and choriocarcinoma.

For research use only. We do not sell to patients.

YTHDF2-IN-1

YTHDF2-IN-1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Description

YTHDF2-IN-1 (Compound CK-75) is a selective YTHDF2 inhibitor (Kd = 26.2 μM). YTHDF2-IN-1 binds to a small hydrophobic pocket on the YTH domain of YTHDF2, disrupting the interaction between YTHDF2 and m6A-modified RNA. YTHDF2-IN-1 induces cell cycle arrest and Apoptosis. YTHDF2-IN-1 is applicable to research on chronic myeloid leukemia, colon cancer and choriocarcinoma[1].

IC50 & Target[1]

YTHDF2

26.2 μM (Kd)

In Vitro

YTHDF2-IN-1 (100 μM; 30 min) inhibits the interaction between the purified YTHDF2 YTH domain and m6A RNA in FP assays, with an inhibition rate of 82.3% at a concentration of 100 μM[1].
YTHDF2-IN-1 binds to the purified YTH domain of YTHDF2 in MST assays, with a Kd value of 26.2 μM[1].
YTHDF2-IN-1 (10-25 μM; 24 h) induces concentration-dependent G0/G1 cell cycle arrest in K562 cells[1].
YTHDF2-IN-1 (25-100 μM; 24 h) induces concentration-dependent apoptosis in K562 cells[1].
YTHDF2-IN-1 (0.4-100 μM; 72 h) exhibits micromolar cytotoxicity against K562, HCT116 and JAR cancer cells in MTT assays, with corresponding IC50 values of 29.7 μM, 33.3 μM and 47.5 μM after 72 h of treatment[1].

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

Cell Cycle Analysis[1]

Cell Line: K562 human cancer cells
Concentration: 10-25 μM
Incubation Time: 24 h
Result: Caused >70% of cells to accumulate in the G0/G1 phase at 25 μM.
Induced concentration-dependent G0/G1 phase cell cycle arrest.

Apoptosis Analysis[1]

Cell Line: K562 human cancer cells
Concentration: 25, 50, 100 μM
Incubation Time: 24 h
Result: Induced total apoptosis in 28.2% of cells at 25 μM, 34.9% at 50 μM, and 45.4% at 100 μM.
Molecular Weight

358.35

Formula

C21H14N2O4

Appearance

Solid

Color

Yellow to orange

SMILES

O=C(O)C1=CC=C(N2N=CC(C(C3=C4C=CC=CC4=CC=C3O)=O)=C2)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 : 50 mg/mL (139.53 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 2.7906 mL 13.9528 mL 27.9057 mL
5 mM 0.5581 mL 2.7906 mL 5.5811 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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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 2.7906 mL 13.9528 mL 27.9057 mL 69.7642 mL
5 mM 0.5581 mL 2.7906 mL 5.5811 mL 13.9528 mL
10 mM 0.2791 mL 1.3953 mL 2.7906 mL 6.9764 mL
15 mM 0.1860 mL 0.9302 mL 1.8604 mL 4.6509 mL
20 mM 0.1395 mL 0.6976 mL 1.3953 mL 3.4882 mL
25 mM 0.1116 mL 0.5581 mL 1.1162 mL 2.7906 mL
30 mM 0.0930 mL 0.4651 mL 0.9302 mL 2.3255 mL
40 mM 0.0698 mL 0.3488 mL 0.6976 mL 1.7441 mL
50 mM 0.0558 mL 0.2791 mL 0.5581 mL 1.3953 mL
60 mM 0.0465 mL 0.2325 mL 0.4651 mL 1.1627 mL
80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8721 mL
100 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6976 mL
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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.

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Product Name:
YTHDF2-IN-1
Cat. No.:
HY-173008
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