Wee1/HDAC-IN-1
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML).
For research use only. We do not sell to patients.
- CAS No.: 3037071-29-4
- Formula: C33H43N9O4
- Molecular Weight:629.75
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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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Wee1 1.2 nM (IC50) |
HDAC1 196 nM (IC50) |
HDAC3 156 nM (IC50) |
HDAC6 55 nM (IC50) |
HDAC2 >2000 nM (IC50) |
HDAC8 1295 nM (IC50) |
HDAC10 1310 nM (IC50) |
HDAC11 >2000 nM (IC50) |
Wee1/HDAC-IN-1 (Compound 23f) (72 h) exhibits strong antiproliferative activity in different AML cell types. Wee1/HDAC-IN-1 against MV4-11 cells, THP-1 cells and HL-60 cells with IC50 values of 0.076 μM, 0.773 μM and 0.309 μM, respectively[1].
Wee1/HDAC-IN-1 (10-75 nM; 96 h) has differentiation-inducing ability in MV4-11 cells[1].
Wee1/HDAC-IN-1 (37.5-600 nM; 72 h) induces cell apoptosis in a dose-dependent manner in MV4-11 cells[1].
Wee1/HDAC-IN-1 (19-1200 nM; 72 h) dose-dependently reduced the phosphorylationlevel of CDK1 while increasing the expression of acetylatedhistone H3. Wee1/HDAC-IN-1 could dose-dependently promote the expression of γH2A.X, a biomarker forDNA double-strand damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11
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Concentration:37.5, 75, 150, 300, 600 nM
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Incubation Time:72 h
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Result:Induced cellapoptosis in a dose-dependent manner, with a notable increasein apoptosis (56.90%) observed at a concentration of 600 nM.
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Cell Line:MV4-11
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Concentration:19, 75, 300, 1200 nM
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Incubation Time:72 h
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Result:Reduced the phosphorylation level of CDK1, increased the expression of acetylated histone H3, and promoted the expression of yH2A.X.
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Cell Line:MV4-11 cells
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Concentration:10, 25, 50, 75 nM
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Incubation Time:96 h
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Result:Induced an increase in CD11b expression,indicating a certain differentiation-inducing ability.
| Species | Dose | Route | Note | Cmax | Tmax | T1/2 | Vd | Clearance (CL) | MRT | Bioavailability | AUC0-t |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat | 2 mg/kg | i.v. | 文献审核 | 912.23 ng/mL | / | 1.94 h | 29.61 L/kg | 10.97 L/h/kg | 1.86 h | / | 184.26 μg/L·h |
| Rat | 10 mg/kg | i.g. | 文献审核 | 8.71 ng/mL | 1.39 h | 2.55 h | 1345.13 L/kg | 750.03 L/h/kg | 4.86 h | 2.21 % | 20.36 μg/L·h |
| Rat | 10 mg/kg | i.p. | 文献审核 | 693.33 ng/mL | 0.16 h | 3.63 h | 21.70 L/kg | 6.78 L/h/kg | 2.60 h | 157.58 % | 1478.93 μg/L·h |
Wee1/HDAC-IN-1 (120-150 mg/kg; i.v; once) shows acceptable hepatic and renal safety profiles in ICR mice (18-20 g)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old) were subcutaneous injection of MV4-11 cells, 1 × 107 cells/mouse[1]
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Dosage:15 mg/kg, 30 mg/kg, 60 mg/kg
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Administration:Intraperitoneal; once daily; 21 days
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Result:Tumor growth was significantly inhibited in a dose-dependent manner.
Median survival time was increased.
Induced significant morphological changes in tumor cells, including cell shrinkage, aggregation, and chromatin marginalization.
\r\nReduced the compensatory CHK1 activation caused by Wee1 inhibition.
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Animal Model:ICR mice (18-20 g)[1]
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Dosage:120 mg/kg, 150 mg/kg
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Administration:Tail vein injection; once
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Result:No significant changes in biochemical parameters (ALT、AST and BUN) or morphological changes in major organs were observed, indicating acceptable hepatic and renal safety profiles and low potential toxicity.
Chemical Information
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CAS No. 3037071-29-4
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Molecular Weight 629.75
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Formula C33H43N9O4
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SMILES
O=C1N(N(C2=NC(NC3=CC=C(C=C3)N4CCN(CC4)CCCCCCC(NO)=O)=NC=C21)C5=NC(C(O)(C)C)=CC=C5)CC=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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