1. PROTAC NF-κB Apoptosis Membrane Transporter/Ion Channel
  2. NF-κB CRM1 PROTACs Apoptosis
  3. PROTAC XPO1 degrader-1

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)).

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

PROTAC XPO1 degrader-1 Chemical Structure

PROTAC XPO1 degrader-1 Chemical Structure

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Description

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673))[1].

In Vitro


PROTAC XPO1 degrader-1 (Compound 2c) effectively degrades XPO1 protein in MV4-11 acute myeloid leukemia (AML) cells with a DC50 of 23.67 nM[1].

PROTAC XPO1 degrader-1 exhibits significant anti-proliferative effects, with IC50 values of 0.142 μM and 0.186 μM against MV4-11 and MOLM-13 cells, respectively[1].

PROTAC XPO1 degrader-1 (100-500 nM; 24 h) effectively induces apoptosis in MV4-11 cells through the caspase pathway[1].

PROTAC XPO1 degrader-1 (100-200 nM; 24 h) can arrest the cell cycle of MV4-11 cells in the G1 phase[1].

PROTAC XPO1 degrader-1 (50 nM; 24 h) reduces cell migration in MV4-11 cells[1].

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

Apoptosis Analysis[1]

Cell Line: MV4-11
Concentration: 100, 200, 500 nM
Incubation Time: 24 h
Result: Induced apoptosis in 71.4 % of the cells at a concentration of 200 nM.
Significantly increased the activation of caspase-3/7 in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: MV4-11
Concentration: 5, 10, 25, 50, 100 ,500 nM
Incubation Time: 12 h
Result: Reduced the protein level of XPO1 in cells in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MV4-11
Concentration: 100, 200 nM
Incubation Time: 24 h
Result: Caused the proportion of cells arrested in the G1 phase to rise from 39.50% to 60.28% as the concentration increased (from 0 to 200 nM).

Cell Migration Assay [1]

Cell Line: MV4-11
Concentration: 50 nM
Incubation Time: 24 h
Result: Resulted in approximately a 42.6 % reduction in MV4-11 cell migration at 50 nM.
Molecular Weight

734.12

Formula

C33H35ClF3N7O7

SMILES

ClC1=C(C(F)(F)F)C=CC(NN2C(C(C)=C(CCC(NCC3CCN(C4=CC=CC(C(NC5C(NC(CC5)=O)=O)=O)=C4OC)CC3)=O)C2=O)=O)=N1

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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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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.

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Product Name:
PROTAC XPO1 degrader-1
Cat. No.:
HY-170669
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