2. Apoptosis
  3. Apoptosis
  4. EXO1-IN-1

EXO1-IN-1 is a human exonuclease 1 (EXO1) inhibitor (IC50 = 15.7 μM). EXO1-IN-1 inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase polyamylation. EXO1-IN-1 induces apoptosis (Apoptosis) in BRCA1-deficient breast cancer cells. EXO1-IN-1 suppresses the growth of BRCA1-deficient breast cancer xenografts. EXO1-IN-1 can be used in research related to BRCA1-deficient breast cancer.

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

EXO1-IN-1

EXO1-IN-1 Chemical Structure

CAS No. : 1111188-09-0

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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

EXO1-IN-1 Related Antibodies

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Description

EXO1-IN-1 is a human exonuclease 1 (EXO1) inhibitor (IC50 = 15.7 μM). EXO1-IN-1 inhibits DNA end resection, promotes the accumulation of DNA double-strand breaks, and triggers S-phase polyamylation. EXO1-IN-1 induces apoptosis (Apoptosis) in BRCA1-deficient breast cancer cells. EXO1-IN-1 suppresses the growth of BRCA1-deficient breast cancer xenografts. EXO1-IN-1 can be used in research related to BRCA1-deficient breast cancer[1].

In Vitro

EXO1-IN-1 (F684) (0-300 μM; overnight treatment) selectively induces replication-associated DNA double-strand breaks and S-phase poly (ADP-ribosylation) in BRCA1-deficient MDA-MB-436 cells[1].
EXO1-IN-1 (20-40 μM; incubated overnight) inhibits replication fork-associated DNA end resection in MDA-MB-231 cells[1].
EXO1-IN-1 (0-100 μM; 48 h) inhibits homology-directed repair of site-specific double-strand DNA breaks (DSBs) and reduces HR frequency in U2OS cells[1].
EXO1-IN-1 (5-50 μM; 5 days) selectively induces apoptosis in BRCA1-deficient human breast cancer cell line MDA-MB-436[1].

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

EXO1-IN-1 Related Antibodies

Immunofluorescence[1]

Cell Line: BRCA1-deficient MDA-MB-436 cells
Concentration: 10, 50 μM
Incubation Time: overnight
Result: Increased the level of DNA damage, elicited a significant increase in γ-H2AX after 24 h.

Western Blot Analysis[1]

Cell Line: BRCA1-deficient MDA-MB-436 cells
Concentration: 0, 50, 100, 200, 300 μM
Incubation Time: overnight
Result: Increased the level of DNA damage, elicited a significant increase in γ-H2AX.

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231 cells
Concentration: 20, 40 μM
Incubation Time: overnight
Result: Reduced the CPT-induced P-RPA levels

Apoptosis Analysis[1]

Cell Line: BRCA1-/+ deficient MDA-MB-436 cells
Concentration: 5, 12, 25, 50 μM
Incubation Time: 5 days
Result: Displays a
substantially stronger killing effect in a BRCA1− context.
In Vivo

EXO1-IN-1 (8.5 mg/kg; i.p.; daily administration, 20 days) significantly slows the growth of BRCA1-deficient human breast cancer xenografts in NSG mice, while exerting no significant effect on xenografts with functional BRCA1[1].

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

Animal Model: NSG (NOD SCID gamma) (6 to 8 week old male or female; xenograft model)[1]
Dosage: 8.5 mg/kg
Administration: i.p.; daily; 20 days
Result: Reduced the average growth rate of BRCA1− tumors.\n
Showed no significant effect on the average growth rate of BRCA1+ tumors.\n
Lowered normalized tumor volume significantly in BRCA1− tumors compared to vehicle controls over the course of the study.\n
Showed no significant difference in normalized tumor volume in BRCA1+ tumors compared to vehicle controls.
Molecular Weight

465.56

Formula

C25H27N3O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(N2CCN(C3=CC=C(NS(=O)(C4=CC=CC=C4)=O)C(C(O)=O)=C3)CC2)C=CC=C1C
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 : 100 mg/mL (214.80 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 2.1480 mL 10.7398 mL 21.4795 mL
5 mM 0.4296 mL 2.1480 mL 4.2959 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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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 2.1480 mL 10.7398 mL 21.4795 mL 53.6988 mL
5 mM 0.4296 mL 2.1480 mL 4.2959 mL 10.7398 mL
10 mM 0.2148 mL 1.0740 mL 2.1480 mL 5.3699 mL
15 mM 0.1432 mL 0.7160 mL 1.4320 mL 3.5799 mL
20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6849 mL
25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1480 mL
30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
80 mM 0.0268 mL 0.1342 mL 0.2685 mL 0.6712 mL
100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 mL
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EXO1-IN-1 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:

EXO1-IN-11111188-09-0ApoptosisEXO1 inhibitorbreast cancerMDA-MB-436 cellsMDA-MB-231 cellsNSG mice
Inhibitorinhibitorinhibit

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