2. GPCR/G Protein
  3. Arf Family GTPase
  4. ART5537

ART5537 is a selective EXO1 inhibitor with a IC50 of 3.4 nM and a Kd of 6.8 nM. ART5537 exerts cellular homologous recombination (HR) inhibition with EC50 of 7.2 nM in HAP1 parental cells. ART5537 shows >200-fold selectivity over a panel of the wider nuclease superfamily. ART5537 exerts biological effects that are exclusively driven by EXO1 inhibition. ART5537 demonstrates sensitization to ionizing radiation and synergy with Olaparib (HY-10162). ART5537 can be used for research in breast cancer and colorectal adenocarcinoma.

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

ART5537

ART5537 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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ART5537 Related Antibodies

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Description

ART5537 is a selective EXO1 inhibitor with a IC50 of 3.4 nM and a Kd of 6.8 nM. ART5537 exerts cellular homologous recombination (HR) inhibition with EC50 of 7.2 nM in HAP1 parental cells. ART5537 shows >200-fold selectivity over a panel of the wider nuclease superfamily. ART5537 exerts biological effects that are exclusively driven by EXO1 inhibition. ART5537 demonstrates sensitization to ionizing radiation and synergy with Olaparib (HY-10162). ART5537 can be used for research in breast cancer and colorectal adenocarcinoma[1].

In Vitro

ART5537 (0.0001-10 μM) displays unambiguous dose-dependent cellular target engagement with an EC50 = 55 nM[1].
ART5537 (0.001-10 μM) has no activation HAP1 EXO1 KO cells, shows no further effect over KO of EXO1 (∼ 50% reduction) and induces a dose-dependent retention of GPF2-EXO1 on chromatin in a U-2 OS Flp-In line [1].
ART5537 (7 days) is not a broadly cytotoxic and has a mild EXO1-dependent sensitivity in MDA-MB-436 (EC50 = 4.0 nM), HCC 1937 (EC50 = 5.3 nM), SUM 149PT (EC50 = 5.0 nM) and HCC38 (EC50 = 8.3 nM) cells[1].
ART5537 (5 days) exhibits no ubiquitous cytotoxicity in HCT116 cells following cotreatment with Olaparib (HY-10162) [1].
ART5537 (7 days) combined with Olaparib exerts a strong synergistic effect in radiation-treated wild-type HCT116 cells, but no such effect is observed in the two radiation-treated EXO1 knockout clones[1].
ART5537 (0.01-100 μM, 6 days) effectively inhibits EXO1, and when combined with Olaparib in radiation-treated HCT116 cells, it significantly enhances the cancer cell-killing effect and greatly increases the activity potency[1].
ART5537 inhibits EXO1 in HCT116 cells and results in a > 40-fold sensitization, has suitable physicochemical properties for use as a cell probe with high thermodynamic solubility and good passive permeability and is unstable in human and mouse liver microsomes[1].

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

ART5537 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT116 cells
Concentration: 0.01, 0.1, 10 and 100 μM
Incubation Time: 6 days
Result: Resulted a > 40-fold sensitization.
Potently sensitized cells irradiated with 3 × 1 Gy (EC50 = 144 nM).
Parmacokinetics
Species Dose Route CL_obs T1/2 Vss
Mice[1] 0.2 mg/kg i.v. 111 mL/min/kg 0.7 h 5.7 L/kg
In Vivo

ART5537 demonstrates unfavorable pharmacokinetic properties in mice, specifically high systemic clearance and very low oral bioavailability (less than 5%)[1].

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

447.87

Formula

C23H18ClN5O3
Appearance

Solid

Color

White to off-white

SMILES

C[C@@H](C1=CC=CC=C1)N2CN(C3=NC=C(Cl)C4=C3C=NC=C4)N5C=CC(C(O)=C5C2=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 : 50 mg/mL (111.64 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 2.2328 mL 11.1640 mL 22.3279 mL
5 mM 0.4466 mL 2.2328 mL 4.4656 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
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 2.2328 mL 11.1640 mL 22.3279 mL 55.8198 mL
5 mM 0.4466 mL 2.2328 mL 4.4656 mL 11.1640 mL
10 mM 0.2233 mL 1.1164 mL 2.2328 mL 5.5820 mL
15 mM 0.1489 mL 0.7443 mL 1.4885 mL 3.7213 mL
20 mM 0.1116 mL 0.5582 mL 1.1164 mL 2.7910 mL
25 mM 0.0893 mL 0.4466 mL 0.8931 mL 2.2328 mL
30 mM 0.0744 mL 0.3721 mL 0.7443 mL 1.8607 mL
40 mM 0.0558 mL 0.2791 mL 0.5582 mL 1.3955 mL
50 mM 0.0447 mL 0.2233 mL 0.4466 mL 1.1164 mL
60 mM 0.0372 mL 0.1861 mL 0.3721 mL 0.9303 mL
80 mM 0.0279 mL 0.1395 mL 0.2791 mL 0.6977 mL
100 mM 0.0223 mL 0.1116 mL 0.2233 mL 0.5582 mL
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ART5537 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:

ART5537ART 5537ART-5537Arf Family GTPaseADP-ribosylation Factor (ARF) Family GTPaseInhibitorinhibitorinhibit

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