2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Wee1 HDAC Apoptosis
  4. 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.

Wee1/HDAC-IN-1

Wee1/HDAC-IN-1 Chemical Structure

CAS No. : 3037071-29-4

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Wee1/HDAC-IN-1 Related Antibodies

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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)[1].

IC50 & Target[1]

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)

In Vitro

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.

Wee1/HDAC-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 37.5, 75, 150, 300, 600 nM
Incubation Time: 72 h
Result: Induced cellapoptosis in a dose-dependent manner, with a notable increasein apoptosis (56.90%) observed at a concentration of 600 nM.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 19, 75, 300, 1200 nM
Incubation Time: 72 h
Result: Reduced the phosphorylation level of CDK1, increased the expression of acetylated histone H3, and promoted the expression of yH2A.X.

Cell Differentiation Assay[1]

Cell Line: MV4-11 cells
Concentration: 10, 25, 50, 75 nM
Incubation Time: 96 h
Result: Induced an increase in CD11b expression,indicating a certain differentiation-inducing ability.
Parmacokinetics
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
In Vivo

Wee1/HDAC-IN-1 (Compound 23f) (15-60 mg/kg; Intraperitoneal; once daily; 21 days) inhibits tumor growth in subcutaneous injection of MV4-11 cells in BALB/c nude[1].
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.

Animal Model: BALB/c nude (female, 6-8 weeks old) were subcutaneous injection of MV4-11 cells, 1 × 107 cells/mouse[1]
Dosage: 15 mg/kg, 30 mg/kg, 60 mg/kg
Administration: Intraperitoneal; once daily; 21 days
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.
Animal Model: ICR mice (18-20 g)[1]
Dosage: 120 mg/kg, 150 mg/kg
Administration: Tail vein injection; once
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.
Molecular Weight

629.75

Formula

C33H43N9O4
CAS No.
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
Shipping

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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Wee1/HDAC-IN-1 Related Classifications

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  • 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:

Wee1/HDAC-IN-13037071-29-4Wee1HDACApoptosisHistone deacetylasesMV4-11 cellsantitumor efficacyxenograft modelhistone deacetylase inhibitorsinhibitory activityCHK1acute myeloid leukemia (AML)dual-targeting compoundsInhibitorinhibitorinhibit

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