2. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  3. Wee1 HSP
  4. HEMTAC WEE1 degrader-1

HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker).

For research use only. We do not sell to patients.

HEMTAC WEE1 degrader-1 Chemical Structure

HEMTAC WEE1 degrader-1 Chemical Structure

CAS No. : 3002417-64-0

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HEMTAC WEE1 degrader-1 Related Antibodies

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Description

HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker)[1].

IC50 & Target

HSP90

16.76 nM (IC50)

In Vitro

HEMTAC WEE1 degrader-1 (Compound 9c) (72 h) inhibits the proliferation activity of MV-4-11 cells (IC50: 8.08 nM) and primary AML cells (IC50: 4.77 nM)[1].
HEMTAC WEE1 degrader-1 (0.01-10 μM, 12 h) degrades WEE1 protein in MV-4-11 cells and has a minor effect on AKT protein, indicating that this effect is independent of HSP90 inhibition[1].
HEMTAC WEE1 degrader-1 (0.1-10 μM, 12 h) promotes the expression of WEE1 mRNA in MV-4-11 cells in a concentration-dependent manner[1].
HEMTAC WEE1 degrader-1 (3-30 nM, 72 h) induces cell cycle arrest at the G2/M phase of MV-4-11 cells in a concentration-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HEMTAC WEE1 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0.01 μM, 0.1 μM, 1 μM and 10 μM
Incubation Time: 12 h
Result: Down-regulated the expression of WEE1 protein.

RT-PCR[1]

Cell Line: MV-4-11 cells
Concentration: 0.1 μM, 1 μM and 10 μM
Incubation Time: 12 h
Result: Up-regulated the expression of WEE1 mRNA.

Cell Cycle Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 3 nM, 10 nM and 30 nM
Incubation Time: 72 h
Result: Induced a large accumulation of cells in the G2/M phase.
In Vivo

HEMTAC WEE1 degrader-1 (Compound 9c) (3 mg/kg, i.v., once every day for 4 weeks) has anticancer activity with minimal toxicity in a mouse AML patient-derived xenograft (PDX) model[1].
HEMTAC WEE1 degrader-1 (10 mg/kg, i.v., once every day for 3 d) has minimal myelosuppressive toxicity in healthy mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: AML patient-derived xenograft (PDX) model, Female NOD/SCID mice (6-9 weeks old)[1]
Dosage: 3 mg/kg
Administration: Intravenous injection (i.v.), once every day for 4 weeks
Result: Reduced the percentage of huCD45-positive cells in the bone marrow (>75%).
Inhibited splenomegaly.
Animal Model: Healthy male BALA/C mice (20-22 g)[1]
Dosage: 10 mg/kg
Administration: Intravenous injection (i.v.), once every day for 3 d
Result: Had minimal effect on platelets, leukocytes and neutrophils
Molecular Weight

1062.27

Formula

C57H71N15O6
CAS No.
SMILES

O=C(C1=NN=C(C2=CC(C(C)C)=C(O)C=C2O)N1C3=CC=C(CN4CCN(CC(NCCCCN5CCN(C6=CC=C(NC7=NC=C8C(N(C9=NC(C(C)(O)C)=CC=C9)N(CC=C)C8=O)=N7)C=C6)CC5)=O)CC4)C=C3)NCC
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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HEMTAC WEE1 degrader-1 Related Classifications

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Help & FAQs
  • 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:

HEMTAC WEE1 degrader-13002417-64-0Wee1HSPHeat shock proteinsAnticancerMV-4-11 cellsAMLAML patient-derived xenograft (PDX) modelInhibitorinhibitorinhibit

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