JAK/HDAC-IN-2
JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.
For research use only. We do not sell to patients.
- CAS No.: 3029138-43-7
- Formula: C28H38N6O5S
- Molecular Weight:570.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JAK2 5.32 nM (IC50) |
JAK1 27.15 nM (IC50) |
JAK3 594.8 nM (IC50) |
Tyk2 414.4 nM (IC50) |
HDAC 170 nM (IC50) |
HDAC1 340 nM (IC50) |
HDAC2 303 nM (IC50) |
HDAC3 58.7 nM (IC50) |
HDAC6 4.44 nM (IC50) |
HDAC10 116.1 nM (IC50) |
HDAC11 724.4 nM (IC50) |
HDAC4 >10000 nM (IC50) |
HDAC5 >10000 nM (IC50) |
HDAC7 >10000 nM (IC50) |
HDAC8 >10000 nM (IC50) |
HDAC9 >10000 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.73 μM
Compound: 21
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Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| HEL | IC50 |
0.33 μM
Compound: 21
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Antiproliferative activity against HEL cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against HEL cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| HeLa | IC50 |
2.88 μM
Compound: 21
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Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| HL-60 | IC50 |
2.58 μM
Compound: 21
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Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HL-60 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| K562 | IC50 |
1.87 μM
Compound: 21
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Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| MCF7 | IC50 |
1.83 μM
Compound: 21
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Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
| PC-3 | IC50 |
2.52 μM
Compound: 21
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Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human PC-3 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 37057760] |
JAK/HDAC-IN-2 (compound 21) exhibits great antiproliferative activities against K562, HL-60, and HEL cells (IC50=1.87, 2.26, and 0.33 μM, respectively). JAK/HDAC-IN-2 inhibits the proliferation of four solid tumor cells, MCF-7, HeLa, A549, and PC-3 (IC50=1.83, 2.88, 0.73, and 2.52 μM, respectively)[1].
JAK/HDAC-IN-2 (1, 5 μM; 24 h) possesses excellent proapoptotic activity in HEL cells and moderate proapoptotic activity in A549 cells[1].
JAK/HDAC-IN-2 (1, 5 μM; 24 h) significantly induces the inhibition of histone deacetylation and STAT3 phosphorylation in hematological malignancy HEL cells as well as solid tumor A549 cells by inhibiting both HDAC and JAK[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL cells
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:The apoptotic rates were 37.6% at 1 μM and 81.5% at 5 μM on HEL cells.
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Cell Line:A549 and HEL cells
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:Bviously upgraded the expression level of acetyl-H3 and acetyl-tubulin in A549 cells in a dose-dependent manner.
Reduced the expression level of p-STAT3-Tyr705.
Pharmacokinetic Parameters of LSD1-IN-14 in male Sprague-Dawley rats[1].
| IV (3 mg/kg) | PO (15 mg/kg) | |
| Tmax (h) | 2.912 | |
| Cmax (ng/mL) | 93.328 | |
| AUC0-t (ng/mL∗h) | 656.241 | 745.249 |
| t1/2 (h) | 0.128 | 2.084 |
| CL (L/ kg∗h) | 4.571 | 4.56 |
| Vss (L/kg) | 0.845 | |
| F (%) | 22.71% |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 nude mice[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneally; once a day for 18 consecutive days
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Result:Prominently reduced the weight and volume of HEL and A549 xenografts.
Upgraded the expression level of acetyl-H3 as well as acetyl-tubulin and reduced the expression level of p-STAT3-Tyr705 in HEL as well as A549 xenograft tumor tissues.
Chemical Information
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CAS No. 3029138-43-7
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Molecular Weight 570.70
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Formula C28H38N6O5S
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SMILES
CC(NS(C1=CC(NC2=NC(NC3=CC=C(C=C3)OCCCCCCC(NO)=O)=NC=C2C)=CC=C1)(=O)=O)(C)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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