2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis PI3K/Akt/mTOR NF-κB
  3. HSP Apoptosis PI3K Akt NF-κB
  4. WK88-1

WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases.

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WK88-1

WK88-1 Chemical Structure

CAS No. : 958888-32-9

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WK88-1 Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases[1][2][3][4][5].

IC50 & Target[1]

HSP90

 

In Vitro

WK88-1 (0.078-100 μM; 24-72 h) potently inhibits proliferation of human ER-positive MCF-7 breast cancer cells[1].
WK88-1 (50.0 μM; 48 h) induces G2/M phase cell cycle arrest in human ER-positive MCF-7 breast cancer cells and human ER-negative MDA-MB-231 breast cancer cells, associated with downregulation of CDK1 and cyclin B1 proteins[1].
WK88-1 (0.1-5 μM; 24 h) inhibits Hsp90 function in gefitinib-resistant H1975 (EGFRL858R/T790M) cells, inducing dose-dependent degradation of oncogenic receptor tyrosine kinases (EGFR, ErbB2, ErbB3, Met) and downstream signaling proteins (Akt), while upregulating Hsp70[2].
WK88-1 (0.5-1 μM; 24 h) induces dose-dependent early apoptosis in gefitinib-resistant H1975 (EGFRL858R/T790M) cells, with early apoptosis reaching 22.23% at 1 μM[2].
WK88-1 (1-5 μM; 24 h) potently suppresses the migration of gefitinib-sensitive HCC827 and gefitinib-resistant Met-amplified HCC827GR non-small cell lung cancer cells[3].
WK88-1 (1-5 μM; 48 h) potently suppresses the invasion of gefitinib-sensitive HCC827 and gefitinib-resistant Met-amplified HCC827GR non-small cell lung cancer cells[3].
WK88-1 (1 μg/mL; 48 h) inhibits 27-hydroxycholesterol-induced transcription of M1 cytokines CXCL10, CXCL11, and TNF-α in THP-1 human monocytic cells[4].
WK88-1 (1 μg/mL; 4 h) inhibits 27-hydroxycholesterol-induced Akt phosphorylation in THP-1 human monocytic cells[4].

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

WK88-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: human ER-positive MCF-7 breast cancer cells, human ER-negative MDA-MB-231 breast cancer cells
Concentration: 1.25-50 μM (flow cytometry); 3.125-50 μM (western blot analysis)
Incubation Time: 48 h (flow cytometry)
Result: Increased the proportion of cells in the G2/M phase by 37.2% in MCF-7 cells and 39.4% in MDA-MB-231 cells at 50.0 μM compared to vehicle controls.
Downregulated the levels of cell cycle regulatory proteins CDK1 and cyclin B1 in both cell lines.

Apoptosis Analysis[1]

Cell Line: human ER-positive MCF-7 breast cancer cells, human ER-negative MDA-MB-231 breast cancer cells
Concentration: 3.125-50 μM (DAPI staining); 50 μM (PI flow cytometry); 3.125-50 μM (Annexin V/PI dual staining)
Incubation Time: 48 h
Result: Induced concentration-dependent nuclear condensation and apoptotic bodies in both cell lines via DAPI staining.
Detected apoptosis rates of 43.8% in MCF-7 cells and 31.6% in MDA-MB-231 cells at 50.0 μM.
Showed late apoptotic cell proportions of 34.9% in MCF-7 cells and 27.9% in MDA-MB-231 cells at 25.0 μM.
Caused no obvious change in early apoptotic cell proportions across tested concentrations compared to controls.

Cell Migration Assay [3]

Cell Line: gefitinib-sensitive HCC827 non-small cell lung cancer cells, gefitinib-resistant HCC827GR (Met-amplified) non-small cell lung cancer cells
Concentration: 1 μM, 5 μM
Incubation Time: 24 h
Result: Strongly abrogated the migratory capacity of both HCC827 and HCC827GR cells in a concentration-dependent manner.
Caused statistically significant inhibition of migration at both 1 μM and 5 μM compared to vehicle controls.

Cell Invasion Assay[3]

Cell Line: gefitinib-sensitive HCC827 non-small cell lung cancer cells, gefitinib-resistant HCC827GR (Met-amplified) non-small cell lung cancer cells
Concentration: 1 μM, 5 μM
Incubation Time: 48 h
Result: Potently inhibited the invasive capacity of both HCC827 and HCC827GR cells in a concentration-dependent manner.
Caused statistically significant inhibition of invasion at both 1 μM and 5 μM compared to vehicle controls.
In Vivo

WK88-1 causes no detectable hepatotoxicity in C57BL/6 mice[1].
WK88-1 (1 mg/kg; injection; 3 times/week) produces significant antitumor efficacy in athymic nude mice bearing H1975 xenografts, with reductions in tumor volume and weight[2].
WK88-1 (1 mg/kg; i.p.; three times per week) significantly inhibits the growth of gefitinib-resistant non-small cell lung cancer xenografts in nude mice, reducing tumor weight by 50%[3].
WK88-1 (10-30 mg/kg; i.v.; twice at 24 h intervals) does not induce hepatotoxicity in healthy C57BL/6 mice, as indicated by stable body weight and normal plasma GOT and GPT levels[3].

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

Animal Model: BALB/c-nu athymic nude mice (male, 5 weeks old, subcutaneous xenograft with gefitinib-resistant HCC827GR cells)[3]
Dosage: 1 mg/kg
Administration: i.p.; three times per week
Result: Caused a significant decrease in tumor volume relative to controls, with statistically significant differences observed on day 7, day 10, and day 13.
Reduced tumor weight to ~0.5 g, representing a significant 50% reduction compared to ~1.0 g in control mice.
Molecular Weight

502.64

Formula

C28H42N2O6
CAS No.
SMILES

C/C(C(NC1=CC2=CC=C1)=O)=C/CC[C@H](OC)[C@@H](OC(N)=O)/C(C)=C/[C@H](C)[C@H]([C@@H](OC)C[C@@H](C2)C)O
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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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WK88-1 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:

WK88-1958888-32-9HSPApoptosisPI3KAktNF-κBHeat shock proteinsPhosphoinositide 3-kinasePKBProtein kinase BNuclear factor-κBNuclear factor-kappaBMDA-MB-231 breast cancer cellsbreast cancernon-small cell lung cancerJurkat T cellsMCF-7 breast cancer cellsTHP-1 human monocytic cellsxenograft modelsHCC827GR cellsHCC827 cellsH1975 cellsInhibitorinhibitorinhibit

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