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Cat. No.: HY-181098

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FKA-9i

FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (k_d: 7.387 μM), YBX1 (k_d: 16.52 μM) and RPN1 (k_d: 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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CAS No.: 3060515-85-4
화학식: C₃₀H₂₆F₂N₂O₉S₂
분자량:660.66

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

FKA-9i Chemical Structure

CAS No.: 3060515-85-4

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

CDK1

Caspase 3

Bcl-2

All p38 MAPK Isoforms :

All CDK Isoforms :

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

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.

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.

Chemical Information

CAS No. 3060515-85-4
분자량 660.66
화학식 C₃₀H₂₆F₂N₂O₉S₂
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
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wu R, et al. Design, synthesis, and antitumor activity of novel Flavokawain A derivatives by suppressing LRPPRC-YBX1-RPN1 cascade. Bioorg Chem. 2026;170:109425. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

FKA-9i

All p38 MAPK Isoforms

All CDK Isoforms

All Caspase Isoforms

All Bcl-2 Family Isoforms