1. Metabolic Enzyme/Protease MAPK/ERK Pathway GPCR/G Protein PI3K/Akt/mTOR
  2. Acyltransferase Ras Akt
  3. Rac1-IN-5

Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer.

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Rac1-IN-5

Rac1-IN-5 Chemical Structure

CAS No. : 694515-65-6

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Description

Rac1-IN-5 is a specific, reversible inhibitor of RAC1 (KD = 30 nM). Rac1-IN-5 competes with guanine nucleotides for specific binding to RAC proteins, effectively blocking RAC1 activity and RAC1-dependent cellular functions. Rac1-IN-5 exhibits anti-tumor metastasis effects in vivo and can improve survival. Rac1-IN-5 can be used to study invasive cancers such as triple-negative breast cancer and colon cancer[1].

In Vitro

Rac1-IN-5 (Compound A41) (10 μM, 1 h) blocks RAC1 activation and RAC1-dependent functions in EGF-stimulated NIH/3T3 fibroblasts[1].
Rac1-IN-5 (10 μM) reduces the activity of RAC P29S and RAC1b in NIH-3T3 fibroblasts expressing RAC wild-type (RAC1 WT) or RAC1 oncomutants (RAC1 P29S and RAC1b)[1].
Rac1-IN-5 (0.01-10 μM) reduces RAC1-GTP levels, the over-activation of AKT and the migration area of spheroids, inhibits colony formation (IC50 = 2.1 μM) in TNBC MDA-MB-468 luciferase (Luc) cells[1].
Rac1-IN-5 (10 μM) has anti-invasive properties in human breast CAF spheroids[1].

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

Western Blot Analysis[1]

Cell Line: MDA-MB-468 Luc cells
Concentration: 10 μM
Incubation Time: 1 h
Result: Reduced AKT overactivation, while p44/42 activation remained unchanged.
In Vivo

Rac1-IN-5 (Compound A41) (25 mg/kg, i.p., once a day, 4 weeks) prevents metastasis in a mouse model of TNBC[1].
Rac1-IN-5 (25 mg/kg, i.p., once a day, 15 days) prevents metastasis in invasive cancers in CT26 cellsxenograft BALB/c female mice model[1].

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

Animal Model: TNBC (4 million MDA-MB-468Luc cells) xenograft NMRI nude mice (5-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 4 weeks
Result: Reduced primary tumor regeneration, secondary tumors in the femur, lungs, kidneys, ovaries, and uterus, reduced ex vivo luminescence intensity in the ovaries and uterus.
Animal Model: TNBC (4 million MDA-MB-468Luc cells) xenograft BALB/c female mice (7-8-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 4 weeks
Result: Reduced the frequency of primary tumor regrowth and metastasis, improving survival rates.
Animal Model: CT26 cells (1x106) xenograft BALB/c female mice (7-8-week-old) model[1]
Dosage: 25 mg/kg
Administration: i.p., once a day, 15 days
Result: Reduced the development of lung metastases and liver metastases, improving survival rates.
Molecular Weight

486.60

Formula

C24H26N2O5S2

CAS No.
SMILES

CC1=CC=C(C=C1)SCCC(NC2=CC=C(C=C2)S(NC3=CC(OC)=CC=C3OC)(=O)=O)=O

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  • 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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Rac1-IN-5
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