2. Cell Cycle/DNA Damage Cytoskeleton
  3. PAK Cdc42-binding kinase
  4. Rac/Cdc42-IN-1

Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer.

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

Rac/Cdc42-IN-1

Rac/Cdc42-IN-1 Chemical Structure

CAS No. : 2143950-05-2

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Rac/Cdc42-IN-1 Related Antibodies

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Description

Rac/Cdc42-IN-1, the major phase I metabolite of the oral Rac/Cdc42 inhibitor MBQ-167 (HY-112842) in vivo, is a selective Rac inhibitor. Rac/Cdc42-IN-1 functions by blocking the GTP-binding activation of Rac1, targeting the autophosphorylation of Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 in downstream PAK1/2/3, with an inhibitory effect superior to that of MBQ-167. Rac/Cdc42-IN-1 significantly inhibits cell migration, and suppresses tumor growth and distant metastasis to the lung, liver and kidney in HER2+ breast cancer mouse models. Rac/Cdc42-IN-1 can be used for targeted research on metastatic breast cancer[1].

In Vitro

Rac/Cdc42-IN-1 (M6) (500 nM; 72 h) exerts no significant effect on the cell viability of triple-negative breast cancer cells MDA-MB-231, MDA-MB-468 and HER2-overexpressing breast cancer cells HER2-BM[1].
Rac/Cdc42-IN-1 (0.001-1000 nM; 120 h) shows no significant cytotoxicity against normal human mammary epithelial cells HMEC[1].
Rac/Cdc42-IN-1 (15-1000 nM; 72 h) exerts no significant effect on the viability of HER2-BM cells[1].
Rac/Cdc42-IN-1 (500 nM; 48 h) does not significantly induce apoptosis in MDA-MB-231, MDA-MB-468 and HER2-BM cells (no obvious change in caspase-3/7 activity)[1].
Rac/Cdc42-IN-1 (250 nM; 24 h) significantly inhibits the autophosphorylation of Group 1 PAK (PAK1/2/3) at Thr423/Thr402/Thr436 and Ser141/Ser144/Ser154 sites in HER2-BM cells, and its inhibitory effect is superior to that of the parent drug MBQ-167 (HY-112842)[1].
Rac/Cdc42-IN-1 (25 nM, 250 nM; 24 h) inhibits the migration of HER2-BM cells[1].

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

Rac/Cdc42-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468, HER2-BM
Concentration: 500 nM
Incubation Time: 48 h
Result: Did not significantly alter caspase-3/7 activity in MDA-MB-231, MDA-MB-468 and HER2-BM cells, indicating no obvious induction of apoptosis, whereas MBQ-167 (HY-112842) significantly induced apoptosis at the same concentration.
In Vivo

Rac/Cdc42-IN-1 (M6) (10 mg/kg; i.p.; 5 times per week; for 8 consecutive weeks) inhibits approximately 90% of tumor growth and reduces distant metastases in the lung, liver and kidney by about 90% in a HER2-positive breast cancer orthotopic xenograft model using female severe combined immunodeficiency (SCID) mice[1].

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

Animal Model: Female Severe Combined Immunodeficiency (SCID) mice bearing orthotopic GFP-HER2-BM breast cancer tumors[1]
Dosage: 10 mg/kg
Administration: i.p.; 5 times per week; for 8 consecutive weeks
Result: Significantly inhibited tumor growth by approximately 90% compared with the vehicle-treated group.
Also prevented the development of distal metastases to the lungs, livers, and kidneys by about 90%, showing comparable antitumor and antimetastatic efficacy to the parent compound MBQ-167 (HY-112842) at the same dosage.
Molecular Weight

310.35

Formula

C20H14N4
CAS No.
SMILES

C1(C2=CN=NN2C3=CC4=C(NC5=CC=CC=C54)C=C3)=CC=CC=C1
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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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Rac/Cdc42-IN-1 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:

Rac/Cdc42-IN-12143950-05-2PAKCdc42-binding kinasep21 activated kinasesmyotonic dystrophy kinase-related Cdc42-binding kinasesMRCKRacCdc42Inhibitorinhibitorinhibit

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