2. Immunology/Inflammation Apoptosis Epigenetics GPCR/G Protein
  3. BCL6 MDM-2/p53 Histone Methyltransferase CXCR Apoptosis
  4. WK500B

WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL).

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WK500B

WK500B Chemical Structure

CAS No. : 2253985-29-2

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WK500B Related Antibodies

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

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Description

WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL)[1].

IC50 & Target[1]

CXCR4

 

In Vitro

WK500B (2.5-10 μM; 24 h) dose-dependently and specifically inhibits BCL6 BTB domain-mediated transcriptional repression in 293T cells, with near-complete inhibition at 10 μM[1].
WK500B (2.5-10 μM; 24 h) can reactivate BCL6 target genes (p53, CDKN1A, CXCR4, CD69) in BCL6-dependent SUDHL4 and Farage DLBCL cells in a dose-dependent and specific manner, but has no such effect in Toledo cells that do not express BCL6[1].
WK500B directly binds to the purified BCL6 BTB protein with a KD of 1.61 μM and inhibits the interaction between purified BCL6 BTB protein and SMRT peptide with an IC50 of 1.37 μM[1].
WK500B (24 h) disrupts the colocalization of BCL6 and its corepressor SMRT in SUDHL4 DLBCL cells[1].
WK500B (2.5-10 μM; 24 h) can induce dose-dependent S-phase cell cycle arrest in SUDHL4 diffuse large B-cell lymphoma (DLBCL) cells, with 78% of cells in S phase at a concentration of 10 μM; it can also induce dose-dependent apoptosis, with an apoptosis rate of 66.0% at 10 μM[1].
WK500B (1.25-10 μM; 72 h) selectively inhibits proliferation of BCL6-dependent DLBCL cell lines (SUDHL4, SUDHL6, OCI-Ly7, Farage, DOHH2) with sub- to low-micromolar IC50 values, has minimal effects on normal cell lines, and its antiproliferative activity is dependent on BCL6 expression[1].
WK500B (2 μM; 24 h for single agent, 72 h for combinations) synergizes with PRMT5 inhibitor GSK591 (HY-100235) and EZH2 inhibitor GSK343 (HY-13500) to enhance BCL6 target gene reactivation and antiproliferative activity in SUDHL4 DLBCL cells[1].

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

WK500B Related Antibodies

Real Time qPCR[1]

Cell Line: SUDHL4 DLBCL cells, Farage DLBCL cells, Toledo BCL6-null cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Dose-dependently reactivated expression of p53, CDKN1A, CXCR4, and CD69 at 10 μM in SUDHL4 cells and Farage cells.
Had no effect on expression of these genes at 10 μM in Toledo BCL6-null cells.

Cell Proliferation Assay[1]

Cell Line: DLBCL cell lines (SUDHL4, SUDHL6, OCI-Ly7, Farage, DOHH2), normal cell lines (NCM460, PNT1A, LO2, HAF), SUDHL4 cells transfected with BCL6 shRNA or scramble shRNA
Concentration: 1.25, 2.5, 5, 10 μM
Incubation Time: 72 h
Result: Inhibited proliferation of DLBCL cell lines with IC50 values of 1.93 μM (SUDHL4), 1.10 μM (SUDHL6), 2.16 μM (OCI-Ly7), 1.19 μM (Farage), and 1.52 μM (DOHH2).
Had much weaker effects on normal cell lines, with IC50 values of 13.99 μM (NCM460), 12.61 μM (PNT1A), 21.61 μM (LO2), and 11.02 μM (HAF).
Showed little inhibitory effect across 1.25-10 μM in SUDHL4 cells with BCL6 knockdown, while dose-dependently inhibiting proliferation of scramble shRNA-transfected control cells.

Cell Cycle Analysis[1]

Cell Line: SUDHL4 DLBCL cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced dose-dependent cell cycle arrest at the S phase: 57% S phase at 2.5 μM, 63% S phase at 5 μM, and 78% S phase at 10 μM.

Apoptosis Analysis[1]

Cell Line: SUDHL4 DLBCL cells
Concentration: 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Induced dose-dependent apoptosis: total apoptotic cells (Annexin V-positive) were 4.81% at 2.5 μM, 25.43% at 5 μM, and 66.0% at 10 μM.
Parmacokinetics
Species Dose Route T1/2 Bioavailability
Rat[1] 10 mg/kg p.o. 7.93 h 82.49 %
Rat[1] 5.0 mg/kg i.v. 6.41 h /
In Vivo

WK500B (50 mg/kg; p.o.; daily; 12 days) significantly inhibits germinal center formation, follicular helper T cell proportions, and immunoglobulin affinity maturation in immunized C57BL/6 mice[1].
WK500B (12.5-25 mg/kg; p.o.; daily; 18 days) potently suppresses DLBCL tumour growth in SCID mice, reactivates BCL6 target genes, reduces tumour cell proliferation, and shows no detectable toxicity[1].

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

Animal Model: C57BL/6 (8-week-old male, immunized intraperitoneally with NP-CGG)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 12 days
Result: Reduced the frequency of germinal center B cells (GL7+FAS+B220+) to 0.4%.
Caused a profound loss of germinal centers detected by immunofluorescent staining.
Reduced the proportion of follicular helper T cells (CXCR5+PD1+CD4+).
Decreased titres of high-affinity NP-specific IgG1 (NP5-BSA) and total NP-specific IgG1 (NP23-BSA) in serum.
Animal Model: SCID (6-8-week-old male, injected subcutaneously with 1×107 SUDHL4 cells)[1]
Dosage: 12.5 mg/kg; 25 mg/kg
Administration: p.o.; daily; 18 days
Result: Significantly suppressed tumour growth compared to controls, with reduced tumour weights and volumes.
Reactivated BCL6 target genes (p53, CDKN1A, CXCR4, CD69) in tumour tissue.
Significantly decreased Ki67-positive proliferating tumour cells.
Caused no significant changes in mouse body weight, and no obvious organ damage was detected via histology.
Molecular Weight

500.38

Formula

C22H23BrFN7O
CAS No.
SMILES

N(C1=NC(=NC=C1F)N2C[C@H](C)N[C@H](C)C2)C3=CC=C(NC(=O)C=4N=C(Br)C=CC4)C=C3
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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WK500B 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:

WK500B2253985-29-2BCL6MDM-2/p53Histone MethyltransferaseCXCRApoptosisB-cell lymphoma 6 proteinB-cell lymphoma 5 protein (BCL-5)Zinc finger and BTB domain-containing protein 27Zinc finger protein 51CXC chemokine receptorsC-X-C motif chemokine receptorsapoptosisToledo cellsSUDHL4 DLBCL cellsSMRT peptidediffuse large B cell lymphomaFarage DLBCL cellscell cycle arrestgerminal center293T cellsInhibitorinhibitorinhibit

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