YZZ-24
YZZ-24 is a highly potent and selective STAT3 inhibitor featuring a Ki of 0.26 μM. YZZ-24 directly binds to STAT3 (STAT3 SH2 domain) and effectively inhibits STAT3 phosphorylation at tyrosine 705 (p-STAT3Tyr705) and STAT3 phosphorylation at serine 727 (p-STAT3Ser727), thereby blocking downstream oncogenic signaling and inducing apoptosis, while having minimal impact on upstream kinases. YZZ-24 can be used in colorectal cancer research.
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- 화학식: C20H18N2O4
- 분자량:350.37
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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STAT3 0.26 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
1.99 μM
|
Inhibits HCT-116 cells growth for 48 hours.
Inhibits HCT-116 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| HT-29 | IC50 |
2.67 μM
|
Inhibits HT-29 cells growth for 48 hours.
Inhibits HT-29 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| MCF7 | IC50 |
1.17 μM
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Inhibits MCF7 cells growth for 48 hours.
Inhibits MCF7 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| ASPC1 | IC50 |
1.75 μM
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Inhibits ASPC1 cells growth for 48 hours.
Inhibits ASPC1 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| PANC-1 | IC50 |
1.60 μM
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Inhibits PANC-1 cells growth for 48 hours.
Inhibits PANC-1 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| SW480 | IC50 |
1.03 μM
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Inhibits SW480 cells growth for 48 hours.
Inhibits SW480 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| MDA-MB-231 | IC50 |
1.04 μM
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Inhibits MDA-MB-231 cells growth for 48 hours.
Inhibits MDA-MB-231 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| HpDe6 | IC50 |
6.29 μM
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Inhibits HpDe6 cells growth for 48 hours.
Inhibits HpDe6 cells growth for 48 hours.
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10.1021/acsmedchemlett.6c00161 |
| BT-549 | IC50 |
3.58 μM
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Inhibits BT-549 cells growth for 48 hours.
Inhibits BT-549 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| HIEC6 | IC50 |
11.15 μM
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Inhibits HIEC6 cells growth for 48 hours.
Inhibits HIEC6 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| BXPC-3 | IC50 |
3.67 μM
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Inhibits BXPC-3 cells growth for 48 hours.
Inhibits BXPC-3 cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
| MCF-10A | IC50 |
8.98 μM
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Inhibits MCF-10A cells growth for 48 hours.
Inhibits MCF-10A cells growth for 48 hours.
|
10.1021/acsmedchemlett.6c00161 |
YZZ-24 (48 h) inhibits SW480 and MDA-MB-231 cells at IC50 of 1.03 μM and 1.04 μM, with equivalent tumor cell activity and a broader safety window for normal intestinal epithelial cells (HIEC6) (SI = 10.82) than normal mammary epithelial cells (MCF-10A) (SI = 8.63)[1].
YZZ-24 (100 μM) markedly enhances the thermal stability of STAT3, consistent with a direct binding event[1].
YZZ-24 (1-4 μM; 48 h) binds STAT3, suppresses its phosphorylation and oncogenic signaling to inhibit colorectal cancer cells (SW480 cells)[1].
YZZ-24 (2-6 μM; 24 h) significantly inhibits the migratory capacity of SW480 cells in a concentration-dependent manner[1].
YZZ-24 (0.2-0.8 μM; 48 h) markedly reduces the clonogenic capacity of SW480 cells in a concentration-dependent manner[1].
YZZ-24 (2-6 μM; 48 h) elicits substantial apoptotic cell death in SW480 cells[1].
YZZ-24 (1-5 μM; 48 h) significantly elevates the proportions of early and late apoptotic cells in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW480 cells
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Concentration:1 μM, 2 μM, 3 μM, 4 μM
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Incubation Time:48 h
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Result:Dose-dependently reduced p-STAT3Tyr705 and p-STAT3Ser727.
Exerted no obvious influence on the phosphorylation of STAT1, STAT5 and upstream kinases JAK2, Src, ERK.
Suppressed STAT3 signaling to downregulate Cyclin D1, BCL-2, BCL-xL and Survivin, inhibiting cell proliferation.
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Cell Line:SW480 cells
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Concentration:2 μM, 4 μM, 6 μM
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Incubation Time:24 h
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Result:Robustly reduced SW480 cells migration.
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Cell Line:SW480 cells
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Concentration:0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM
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Incubation Time:48 h
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Result:Significantly reduced the clonogenic capacity of SW480 cells in a concentration-dependent manner.
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Cell Line:SW480 cells
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Concentration:2 μM, 4 μM, 6 μM
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Incubation Time:48 h
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Result:Caused nuclear condensation and fragmentation in SW480 cells upon Hoechst 33342 staining.
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Cell Line:SW480 cells
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Concentration:1 μM, 2 μM, 3 μM, 4 μM, 5 μM
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Incubation Time:48 h
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Result:Significantly increased both early and late apoptotic cell populations in a concentration-dependent manner.
Chemical Information
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분자량 350.37
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화학식 C20H18N2O4
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SMILES
O=C1C(OC2=CC=C(N3CCNCC3)C=C2)=CC(C4=C1C(O)=CC=C4)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YZZ-24 Related Classifications
HY-184419 Related Classifications
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