2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. GSK4418959

GSK4418959 (IDE275) is a selective, reversible and orally active WRN helicase inhibitor. GSK4418959 shows >10,000-fold selectivity over other helicases. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer, such as colorectal cancer (CRC) and endometrial cancer (EC).

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

GSK4418959

GSK4418959 Chemical Structure

CAS No. : 3064599-36-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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GSK4418959 Related Antibodies

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Description

GSK4418959 (IDE275) is a selective, reversible and orally active WRN helicase inhibitor. GSK4418959 shows >10,000-fold selectivity over other helicases. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer, such as colorectal cancer (CRC) and endometrial cancer (EC)[1].

In Vitro

GSK4418959 (0.1-100 µM; 5 days) selectively inhibits the proliferation of MSI-H cells, across different tumor types. Importantly, no response is observed in analogous microsatellite stable (MSS) cells[1].
GSK4418959 (0.001-100 µM) binds to WRN in HCT116 and HT29[1].
GSK4418959 (5 µM) downregulates WRN and upregulates GDF15 in cells. WRN downregulation occurs in both p53 wt (SW48) and mut MSI-H lines (LS411N) but GDF15 upregulation is only observed in SW48 cells[1].

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

GSK4418959 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEC251 (MSS EC), HEC6 (MSI-H EC), SW48 (MSI-H CRC), and SW620 (MSS CRC) cells
Concentration: 0.1 µM, 1 µM, 10 µM, 100 µM
Incubation Time: 5 days
Result: Selectively inhibited the proliferation of MSI-H cells, across different tumor types .
No response was observed in analogous microsatellite stable (MSS) cells.
In Vivo

GSK4418959 (10-100 mg/kg; oral; once daily; 24 days) demonstrates dose-dependent antitutmor activity, including tumor regression in SW48 xenograt tumor models. And no response is observed in analogous microsatellite stable (MSS) models[1].
GSK4418959 (30-300 mg/kg; oral; once daily; 3 days) shows dose-dependent induction of γH2AX, pKAP1, and p21 in SW48 xenograft tumors in a dose-dependent manner[1].

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

Animal Model: SW48 xenograft tumors[1]
Dosage: 10 mg/kg, 50 mg/kg, 100 mg/kg
Administration: Oral; once daily; 24 days
Result: Demonstrated dose-dependent antitutmor activity, including tumor regression in SW48 xenograt tumor models.
No response was observed in analogous microsatellite stable (MSS) models.
Animal Model: SW48 xenograft tumors[1]
Dosage: 30 mg/kg, 100 mg/kg, or 300 mg/kg
Administration: Oral; once daily; 3 days
Result: Showed dose-dependent induction of γH2AX, pKAP1, and p21 in SW48 xenograft tumors in a dose-dependent manner.
Clinical Trial
Molecular Weight

646.65

Formula

C31H30F4N4O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C(F)(F)F)C=C1F)[C@@H]2CCC[C@H](C3=CC=C(N(C)S(=O)(C4=CC(N=C(C)N5C)=C5C=C4)=O)C=C3)[C@H]2C(O)=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 : 100 mg/mL (154.64 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 1.5464 mL 7.7322 mL 15.4643 mL
5 mM 0.3093 mL 1.5464 mL 3.0929 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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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.07%

SDS (251 KB)

COA (249 KB) HNMR (321 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
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 1.5464 mL 7.7322 mL 15.4643 mL 38.6608 mL
5 mM 0.3093 mL 1.5464 mL 3.0929 mL 7.7322 mL
10 mM 0.1546 mL 0.7732 mL 1.5464 mL 3.8661 mL
15 mM 0.1031 mL 0.5155 mL 1.0310 mL 2.5774 mL
20 mM 0.0773 mL 0.3866 mL 0.7732 mL 1.9330 mL
25 mM 0.0619 mL 0.3093 mL 0.6186 mL 1.5464 mL
30 mM 0.0515 mL 0.2577 mL 0.5155 mL 1.2887 mL
40 mM 0.0387 mL 0.1933 mL 0.3866 mL 0.9665 mL
50 mM 0.0309 mL 0.1546 mL 0.3093 mL 0.7732 mL
60 mM 0.0258 mL 0.1289 mL 0.2577 mL 0.6443 mL
80 mM 0.0193 mL 0.0967 mL 0.1933 mL 0.4833 mL
100 mM 0.0155 mL 0.0773 mL 0.1546 mL 0.3866 mL
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GSK4418959 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:

GSK44189593064599-36-3IDE275GSK 4418959GSK-4418959IDE 275IDE-275DNA/RNA SynthesisWRN helicaseATPaseDNA unwinding functionsmicrosatellite instability-high (MSI-H) cancercolorectal cancer (CRC)endometrial cancer (EC)Inhibitorinhibitorinhibit

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