2. PROTAC Protein Tyrosine Kinase/RTK NF-κB
  3. PROTACs Itk NF-κB
  4. BSJ-05-037

BSJ-05-037 是一种 ITK PROTACs 降解剂，能够有效靶向并降解 T 细胞淋巴瘤细胞系中的 ITK。BSJ-05-037 可阻断 NF-κB/GATA-3 信号通路的激活，抑制 PLCγ1 磷酸化，并降低 T 细胞淋巴瘤细胞的增殖能力。BSJ-05-037 能提高 T 细胞淋巴瘤细胞对细胞化疗的敏感性。BSJ-05-037 在小鼠的 T 细胞淋巴瘤模型中诱导 ITK 降解、GATA-3 表达降低，减小肿瘤体积，逆转化疗耐药性。BSJ-05-037 可用于 T 细胞淋巴瘤的相关研究。

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BSJ-05-037

BSJ-05-037 Chemical Structure

CAS No. : 2756388-01-7

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规格 价格 是否有货 数量
5 mg ￥13090
5 - 6 周
10 mg 询价 5 - 6 周
50 mg   询价  
100 mg   询价  

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BSJ-05-037 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BSJ-05-037 is a ITK PROTACs degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma[1][2][3].

IC50 & Target

Cereblon

 

体外研究
(In Vitro)

BSJ-05-037 (0.001-10 μM; 2-16 h) 可在 DERL-2、Hut78 细胞中强效诱导呈时间和浓度依赖性的 ITK 降解，降解具有 CRBN 依赖性[1]。
BSJ-05-037 (1 μM; 10 days) 可强效抑制 DERL-2 和 Jurkat T 细胞淋巴瘤细胞的增殖[1]。
BSJ-05-037 (0.025-0.5 μM; 8 h) 可剂量依赖性地抑制 DERL-2 细胞中 PLCγ1 的磷酸化[1]。
BSJ-05-037 (1 μM; 24 h-3 days) 可阻断 TCR 诱导的 GATA-3 上调，并使 T8ML-1 细胞对 Vincristine (HY-N0488A) 重新增敏，从而克服由 ITK/NF-κB/GATA-3 轴介导的耐药性[1]。
BSJ-05-037 (1 μM; 24 h-4 days) 可在 Hut78 和 H9 皮肤 T 细胞淋巴瘤细胞中诱导近乎完全的 ITK 降解，并使 GATA-3 水平降低 90%以上，同时还能在 4 天的处理过程中增强这些细胞对 Vincristine 的敏感性[1]。

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

BSJ-05-037 相关抗体:

Western Blot Analysis[1]

Cell Line: DERL-2、Hut78 cells
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 2, 4, 8, 16 h
Result: Induced potent degradation of ITK protein in a dose-dependent manner after a 16 h treatment (IC50 = 17.6~ 41.8 nM).

Cell Viability Assay[1]

Cell Line: T-cell lymphoma cell lines (DERL-2, Jurkat)
Concentration: 1 μM
Incubation Time: 10 days
Result: Reduced DERL-2 cell viability to <10% of DMSO control after 10 days.
Induced growth inhibition in Jurkat cells.

Western Blot Analysis[1]

Cell Line: DERL-2 cells
Concentration: 0.025, 0.1, 0.25, 0.5 μM
Incubation Time: 8 h
Result: Resulted in dose-dependent inhibition of PLCγ1 phosphorylation.

Western Blot Analysis[1]

Cell Line: T8ML1 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced potent ITK degradation and abrogated TCR-dependent upregulation of GATA-3.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax
Mice[1] 10 mg/kg i.p. 1.9 h 3.4 μM
体内研究
(In Vivo)

BSJ-05-037 (50 mg/kg; i.p.; every 8 hours; 3 total doses/once every other day; 14 days) 可在小鼠的 Hut78/H9 皮肤 T 细胞淋巴瘤异种移植物中诱导 ITK 降解、GATA-3 表达降低和抑制 PLCγ1，减小肿瘤体积，逆转化疗耐药性[1]。

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

Animal Model: NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ (NSG) mice (9-10 weeks old)[1]
Dosage: 50 mg/kg
Administration: i.p.; every 8 hours; 3 total doses/ once every other day; 14 days
Result: Induced 99.2% degradation of ITK in xenografted tumors.
Reduced GATA-3 protein levels by >90% in treated tumors.
Reduced mean tumor volume to ~1100 mm3 by day 14 as monotherapy.
Achieved almost complete tumor stasis, with mean tumor volume reduced to ~150 mm3 by day 14 when combined with vincristine.
Enriched NF-κB pathway gene.
Downregulated GATA3, IL2, CD69, and the NF-κB regulators NFKBIA.
Resulted in an enrichment of signatures for other TCR pathways including inflammatory response,
STAT3 and STAT5 signaling, MYC targets and cell cycle regulation.
分子量

1022.20

Formula

C51H59N9O10S2
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

BSJ-05-037 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

BSJ-05-0372756388-01-7PROTACsItkNF-κBInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseNuclear factor-κBNuclear factor-kappaBITK PROTACs degraderT-cell lymphomaDERL-2 cellsHut78 cellsT8ML1 cellsNSG mice
Inhibitorinhibitorinhibit

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