HSF1-IN-3
HSF1-IN-3 is a heat shock transcription factor 1 (HSF1) inhibitor with a Kd value of 23.8 μM against HSF1-DBD. HSF1-IN-3 inhibits the proliferation of cancer cells and induces their apoptosis, with stronger activity in androgen-dependent prostate cancer cells. HSF1-IN-3 reduces the expression of HSP70 and HSP90, downstream effectors of HSF1, and attenuates HSE-driven transcriptional activity. HSF1-IN-3 can be used in the research of cancers such as prostate cancer and leukemia.
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- Formule: C18H18BN3
- Masse moléculaire:287.17
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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HSF1 23.8 μM (Kd) |
HSP70 |
HSP90 |
HSF1-IN-3 (Compound 1168) (0.78-25 μM; 30 min) dose-dependently disrupts the formation of purified recombinant human HSF1-DBD/HSE DNA complexes, with nearly complete inhibition observed at 12.5 μM[1].
HSF1-IN-3 (4-20 μM; 72 h) inhibits the proliferation of various cancer cell lines (HCT116, PC-3, LNCaP, 22Rv1, K562, A549, HL60, HeLa), with IC50 values ranging from 7.5 μM (HL60) to 19.5 μM (HeLa) after 72 h of treatment; meanwhile, the IC50 value of this compound in non-cancerous HEK293 cells is 4-fold higher, indicating a potential therapeutic window[1].
HSF1-IN-3 (2.5-20 μM; 10 days) inhibits the long-term clonogenic capacity of 22Rv1 prostate cancer cells in a dose-dependent manner[1].
HSF1-IN-3 (5-20 μM; 48 h) activates the caspase-dependent apoptotic signaling pathway in HL60 leukemia cells in a dose- and time-dependent manner[1].
HSF1-IN-3 (5-20 μM; 7-48 h) dose-dependently inhibits the expression of HSF1 and its downstream effector proteins (HSP70, HSP90, Akt) in HL60 leukemia cells and 22Rv1 prostate cancer cells under both basal and heat shock conditions. In addition, it reduces the level of androgen receptor in 22Rv1 cells[1].
HSF1-IN-3 (5-20 μM; 7 h) dose-dependently inhibits HSE-mediated transcriptional activity in HEK293T cells, with an inhibition rate of approximately 70% at the concentration of 20 μM after heat shock treatment[1].
HSF1-IN-3 (5-20 μM; 7 h) dose-dependently attenuates heat shock-induced phosphorylation of HSF1 Ser326 in 22Rv1 prostate cancer cells[1].
HSF1-IN-3 (5-20 μM; 7 h) dose-dependently attenuates heat shock-induced phosphorylation of HSF1 Ser326 in HL60 leukemia cells, and this effect is independent of its downregulatory action on total HSF1 protein levels[1].
HSF1-IN-3 (5-20 μM; 7 h) dose-dependently reduces the abundance of HSF1 trimers in heat shock-induced HL60 leukemia cells, and this effect is partially mediated by the proteasome-dependent degradation of HSF1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL60 cells
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Concentration:2.5, 5, 10 and 20 μM
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Incubation Time:10 days
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Result:Dose-dependently impaired the long-term clonogenic growth of 22Rv1 prostate cancer cells, with near-complete inhibition at 20 μM after 10 days.
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Cell Line:HL60 cells
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Concentration:5, 10 and 20 μM
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Incubation Time:48 and 72 h
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Result:Induced time-dependent apoptosis in HL60 leukemia cells, with 75.60% early apoptosis at 20 μM after 48 h and 83.39% late apoptosis at 20 μM after 72 h.
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Cell Line:HL60 cells
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Concentration:5, 10 and 20 μM
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Incubation Time:Basal conditions for 48 h or under heat shock conditions (2 h pretreatment, 1 h at 43 ◦C, followed by 4 h
recovery) -
Result:Dose-dependently suppressed the expression of HSF1 and its downstream effector proteins (HSP70, HSP90, Akt) in HL60 leukemia cells and 22Rv1 prostate cancer cells under both basal and heat shock conditions, and additionally reduced androgen receptor levels.
Chemical Information
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Masse moléculaire 287.17
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Formule C18H18BN3
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SMILES
CN(C=CN1C)C1BC2=NC3=C(C=CC=C3)C4=C2C=CC=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HSF1-IN-3 Related Classifications
HY-184309 Related Classifications
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