1. Protein Tyrosine Kinase/RTK Apoptosis
  2. Anaplastic lymphoma kinase (ALK) Apoptosis
  3. W23-1006

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC).

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

W23-1006 Chemical Structure

W23-1006 Chemical Structure

CAS No. : 3035498-92-8

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Description

W23-1006 is a selective and covalent ALKBH5 inhibitor. W23-1006 binds to the ALKBH5 C200 residue with an IC50 value of 3.848 μM. W23-1006 shows ~30- and 8-fold stronger inhibitory activity than that against FTO and ALKBH3, respectively. W23-1006 can be used for the study of triple-negative breast cancer (TNBC)[1].

In Vitro

W23-1006 (5 μM; 24 h) significantly increases the mA abundance in MDA-MB-231 and BT549 cells[1].
W23-1006 (3.16-31.6 μM; 24 h) inhibits the cell viability of MDA-MB-231 and BT549[1].
W23-1006 (5 μM) could obviously reduce TNBC cell colonization area and suppress cell migration[1].
W23-1006 (5-10 μM) induces the apoptosis and decreases the G2/M phase of MDA-MB-231 cells[1].

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

RT-PCR[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 5 μM
Incubation Time: 24 h
Result: The mA abundance significantly increased in cells.

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and BT549 cells
Concentration: 3.16 μM, 10 μM, 31.62 μM
Incubation Time: 24 h
Result: Inhibited cell viability of MDA-MB-231 and BT549 with IC50 values of 10.31 μM and 6.338 μM, respectively.
In Vivo

W23-1006 (25 mg/kg; intraperitoneal injection (i.p.); once daily; for 14 days) exerts antitumor efects on breast cancer in vivo[1].
W23-1006 (25 mg/kg; i.p.; once daily; for 10 days) could obviously inhibit TNBC lung metastasis[1].
W23-1006 (single dosage at 25 mg/kg; i.p.) shows the t1/2 ranged from 0.509 to 0.983 h, and the Cmax in plasma (in the range of 1715-2108 ng/mL) is reached 15 min in mice[1].
Neither 100 mg/kg nor 250 mg/kg dosage of W23-1006 (i.p.) causes adverse events or death in KM mice (22-27g)[1].

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

Animal Model: Immunodefcient female mouse was subcutaneously injected MDA-MB-231 cells[1].
Dosage: 25 mg/kg (5% DMSO, 10% Kolliphor HS 15, and 85% saline)
Administration: Intraperitoneal injection; once daily; for 14 days
Result: Apparently reduced the tumor volume and weight.
Strongly reduced the FN1 and Ki-67 protein expression level.
Animal Model: Immunodefcient female mouse injected MDA-MB-231LMF3 through the tail vein[1].
Dosage: 25 mg/kg
Administration: Intraperitoneal injection; once daily; for 10 days
Result: Inhibited TNBC lung metastasis.
No apparent pathologic abnormality was observed in the HEstaining results of multiple organs, including heart, liver,spleen, lung, and kidney.
There was no signifcant diference in glutamic pyruvic transaminase(ALT) and glutamic oxaloacetic transaminase (AST) levels in mouse serum, did not infuence mice liver function.
Molecular Weight

418.20

Formula

C17H12BrN3O5

CAS No.
SMILES

O=C(/C1=C\C2=CC([N+]([O-])=O)=CC(Br)=C2)NN(C3=CC=C(C=C3)OC)C1=O

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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.

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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:
W23-1006
Cat. No.:
HY-173020
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