2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis MAPK/ERK Pathway Cell Cycle/DNA Damage
  3. Reactive Oxygen Species (ROS) Apoptosis p38 MAPK CDK Caspase Bcl-2 Family
  4. FKA-9i

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (kd: 7.387 μM), YBX1 (kd: 16.52 μM) and RPN1 (kd: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer.

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FKA-9i

FKA-9i Chemical Structure

CAS No. : 3060515-85-4

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FKA-9i Related Antibodies

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Description

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (kd: 7.387 μM), YBX1 (kd: 16.52 μM) and RPN1 (kd: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer[1].

IC50 & Target[1]

CDK1

 

Caspase 3

 

Bcl-2

 

In Vitro

FKA-9i (0-72 h) inhibits the proliferation of HGC27, KYSE70, KYSE450, HCT116 and A549 cancer cells, with IC50 values of 1.49, 3.15, 2.25, 3.53 and 4.48 μM, respectively[1].
FKA-9i (0-8 μM; 0-48 h) inhibits tumor cell proliferation, and induces cell cycle arrest and apoptosis[1].
FKA-9i (0-8 μM; 0-48 h) reduces the stability of LRPPRC, YBX1 and RPN1 proteins in HGC27 cells and promotes their degradation[1].
FKA-9i (48 h) inhibits the expression of genes related to the MAPK signaling pathway and suppresses the MAPK cascade in HGC27 cells[1].
FKA-9i (4-8 μM; 48 h) dose-dependently increases intracellular ROS levels in HGC27 and HCT116 cells[1].

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

FKA-9i Related Antibodies

Cell Cycle Analysis[1]

Cell Line: HGC27, KYSE450, HCT116
Concentration: 0, 2, 4 and 8 μM
Incubation Time: 48 h
Result: Induced G1 phase arrest in HGC27 and HCT116 cells, and S phase arrest in KYSE450 cells.
Downregulated cell cycle regulators CCND1 and CDK1.

Western Blot Analysis[1]

Cell Line: HGC27, KYSE450, HCT116
Concentration: 0, 2, 4 and 8 μM
Incubation Time: 48 h
Result: Reduced protein expression levels of caspase-3 and anti-apoptotic protein Bcl-2.
In Vivo

FKA-9i (2.5-5 mg/kg; oral gavage; 31 days) exhibits anti-tumor activity in the HGC27 CDX mouse model[1].
FKA-9i (100-200 mg/kg; oral gavage; 10 days) shows no obvious acute organ toxicity in C57BL/6 mice[1].

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

Animal Model: BALB/c-nu nude mice (female, 6-week-old) treated HGC27 cells[1]
Dosage: 2.5 mg/kg/day; 5 mg/kg/day
Administration: Oral gavage; 31 days
Result: Reduced mean tumor volume, tumor number, and tumor weight.
Showed no significant differences in body weight compared to the control group.
Animal Model: C57BL/6 mice (male, 8-week-old)[1]
Dosage: 100 mg/kg/day; 200 mg/kg/day
Administration: Oral gavage; 10 days
Result: Showed no significant differences in body weight organ weights compared to the control group.
Observed no histopathological changes (H&E staining of liver and kidney tissues) compared to the control group.
Molecular Weight

660.66

Formula

C30H26F2N2O9S2
CAS No.
SMILES

COC1=CC(OC)=C(C(CC(C2=CC(S(NC3=CC=C(F)C=C3)(=O)=O)=C(OC)C=C2)O4)=O)C4=C1S(NC5=CC=C(F)C=C5)(=O)=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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FKA-9i 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:

FKA-9i3060515-85-4Reactive Oxygen Species (ROS)Apoptosisp38 MAPKCDKCaspaseBcl-2 FamilyCyclin dependent kinaselung cancerLRPPRCcolon cancerHGC27MAPKYBX1gastric cancerInhibitorinhibitorinhibit

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