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

WK500B 是一种高效且口服有效的 BCL6 抑制剂，解离常数 (KD) 为 1.61 μM。WK500B 可结合细胞内的 BCL6，破坏 BCL6- 辅抑制因子的相互作用，从而重新激活 BCL6 靶基因。WK500B 对弥漫性大 B 细胞淋巴瘤细胞具有细胞毒性，可诱导凋亡 (apoptosis) 和周期阻滞。WK500B 可抑制 C57BL/6 小鼠的生发中心形成，还可抑制 SCID 异种移植模型中的 DLBCL 肿瘤生长，且无明显毒性。WK500B 可用于弥漫性大 B 细胞淋巴瘤 (DLBCL) 的研究。

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WK500B

WK500B Chemical Structure

CAS No. : 2253985-29-2

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WK500B 相关抗体

Top Publications Citing Use of Products

查看 Histone Methyltransferase 亚型特异性产品:

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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CXCR CXCR1 CXCR2 CXCR3 CXCR4 CXCR7 CXCR6

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

WK500B (2.5-10 μM; 24 h) 可在 293T 细胞中呈剂量依赖性且特异性地抑制 BCL6 BTB 结构域介导的转录抑制，在 10 μM 时抑制作用接近完全[1]。
WK500B (2.5-10 μM; 24 h) 能在 BCL6 依赖型 SUDHL4 和 Farage DLBCL 细胞中呈剂量依赖性且特异性地重新激活 BCL6 靶基因 (p53、CDKN1A、CXCR4、CD69)，而在不表达 BCL6 的 Toledo 细胞中无此作用[1]。
WK500B 可直接与纯化的 BCL6 BTB 蛋白结合，其 KD 为 1.61 μM；还可抑制纯化的 BCL6 BTB 蛋白与 SMRT 肽之间的相互作用，其 IC50 为 1.37 μM[1]。
WK500B (孵育 24 h) 可破坏 SUDHL4 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞中 BCL6 与其共抑制因子 SMRT 的共定位[1]。
WK500B (2.5-10 μM; 24 h) 可在 SUDHL4 弥漫大 B 细胞淋巴瘤 (DLBCL) 细胞中诱导剂量依赖性 S 期细胞周期阻滞，10 μM 浓度下 S 期细胞比例达 78%；同时可诱导剂量依赖性凋亡，10 μM 时细胞凋亡率为 66.0%[1]。
WK500B (1.25-10 μM; 72 h) 可选择性抑制依赖 BCL6 的 DLBCL 细胞系 (SUDHL4、SUDHL6、OCI-Ly7、Farage、DOHH2) 的增殖，其 IC50 值介于亚微摩尔至低微摩尔水平，对正常细胞系的影响极小，且其抗增殖活性依赖于 BCL6 的表达[1]。
WK500B (2 μM; 24 h for single agent, 72 h for combinations) 可与 PRMT5 抑制剂 GSK591 (HY-100235) 及 EZH2 抑制剂 GSK343 (HY-13500) 产生协同作用，增强 SUDHL4 弥漫性大 B 细胞淋巴瘤 (DLBCL) 细胞中 BCL6 靶基因的再激活及抗增殖活性[1]。

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

WK500B 相关抗体:

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.
药代动力学
(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 /
体内研究
(In Vivo)

WK500B (50 mg/kg；口服；每日；12 天) 可显著抑制经免疫的 C57BL/6 小鼠的生发中心形成、滤泡辅助性 T 细胞比例以及免疫球蛋白亲和力成熟[1]。
WK500B (12.5-25 mg/kg；口服；每日一次；连续 18 天) 可强效抑制 SCID 小鼠体内的 DLBCL 肿瘤生长，重新激活 BCL6 靶基因，降低肿瘤细胞增殖能力，且未检测到毒性[1]。

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.
分子量

500.38

Formula

C22H23BrFN7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

WK500B 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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