2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. WRN-IN-24

WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer.

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

WRN-IN-24

WRN-IN-24 Chemical Structure

CAS No. : 3113010-46-8

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WRN-IN-24 Related Antibodies

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Description

WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer[1].

IC50 & Target[1]

Helicase

 

In Vitro

WRN-IN-24 (Compound 22) potently inhibits purified WRN helicase activity with an IC50 of 201 nM[1].
WRN-IN-24 potently inhibits the proliferation of HCT116 MSI-H colorectal cancer cells with an IC50 of 49 nM[1].
WRN-IN-24 activates the DNA damage response marker γH2AX in SW48 MSI-H colorectal cancer cells with an EC50 of 338 nM[1].
WRN-IN-24 potently inhibits the proliferation of SW48 MSI-H colorectal cancer cells with an IC50 of 48.0 nM[1].
WRN-IN-24 shows no proliferation inhibitory activity against HT29 and MDA-MB-231 MSS cell lines, with IC50 values > 10000 nM for both[1].

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

WRN-IN-24 Related Antibodies
Parmacokinetics
Species Dose Route CL Vdss T1/2 Cmax AUC0-last F
Mice[1] 1 mg/kg i.v. 0.82 L/h/kg 3.36 L/kg 3.20 h / / /
Mice[1] 10 mg/kg p.o. / / / 1393 ng/mL 10152 ng·h/mL 98.1 %
Rat[1] 1 mg/kg i.v. 0.70 L/h/kg 2.63 L/kg 4.42 h / / /
Rat[1] 10 mg/kg p.o. / / / 782 ng/mL 7751 ng·h/mL 55.5 %
Dog[1] 1 mg/kg i.v. 0.11 L/h/kg 4.37 L/kg 28.8 h / / /
Dog[1] 5 mg/kg p.o. / / / 869 ng/mL 14960 ng·h/mL 71.5 %
Monkey[1] 1 mg/kg i.v. 0.20 L/h/kg 1.54 L/kg 5.89 h / / /
Monkey[1] 5 mg/kg p.o. / / / 1267 ng/mL 19069 ng·h/mL 82.6 %
In Vivo

WRN-IN-24 (Compound 22) (5-20 mg/kg; p.o.; daily for 21 days) inhibits tumor growth in the HCT116 (MSI-H) xenograft mice models[1].

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

Animal Model: Mice HCT116 (MSI-H) xenograft[1]
Dosage: 5, 10 and 20 mg/kg
Administration: P.o.; daily for 21 days
Result: Inhibited tumor growth with TGI of 95.2% at 20 mg/kg.
Molecular Weight

603.63

Formula

C24H28F3N5O6S2
CAS No.
SMILES

O=C(C1=C(OC2=CC=CC=C2)N=C(C(F)(F)C)N=C1NC3CN(S(=O)(C)=O)C3)N[C@@H](C4CC4)/C=C(F)/S(=O)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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WRN-IN-24 Related Classifications

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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.

Keywords:

WRN-IN-243113010-46-8DNA/RNA SynthesisSW48 MSI-H colorectal cancer cellsK894colorectal cancerHT29 MSS cell linesHCT116 MSI-H colorectal cancer cellsmicrosatellite instability-high cancersMDA-MB-231 MSS cell linesxenograft mouse modelscolorectal cancer cellsWerner syndrome helicaseInhibitorinhibitorinhibit

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