2. Immunology/Inflammation Stem Cell/Wnt MAPK/ERK Pathway NF-κB
  3. IRAK Toll-like Receptor (TLR) ERK NF-κB Interleukin Related
  4. BMS-986126

BMS-986126 是一种强效、选择性强且口服有效的 IRAK4 抑制剂 (IC50 = 5.3 nM) 。BMS-986126 可广泛抑制 MyD88 依赖性信号通路。BMS-986126 在 MRL/lpr 和 NZB/NZW 小鼠狼疮模型中表现出显著的活性，可抑制多种致病反应。BMS-986126 可用于自身免疫性疾病的相关研究，例如系统性红斑狼疮 (SLE)。

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BMS-986126

BMS-986126 Chemical Structure

CAS No. : 1610017-20-3

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BMS-986126 相关抗体

Top Publications Citing Use of Products

查看 IRAK 亚型特异性产品:

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IRAK1 IRAK4

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TLR3 TLR8 TLR9 TLR2 TLR4 TLR7 TLR1 TLR6

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ERK ERK1 ERK2 ERK5 ERK8

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-986126 is a potent, selective, and orally active IRAK4 inhibitor (IC50 = 5.3 nM). BMS-986126 broadly inhibits MyD88-dependent signaling pathways. BMS-986126 demonstrates robust activity in the MRL/lpr and NZB/NZW murine models of lupus, inhibiting multiple pathogenic responses. BMS-986126 can be used for autoimmune diseases research, such as lupus erythematosus (SLE)[1].

IC50 & Target[1]

IRAK4

5.3 nM (IC50)

体外研究
(In Vitro)

BMS-986126 对人外周血单核细胞 (PBMC) 中多种 MyD88 依赖性 TLR (TLR2/5/7/9) 表现出相似的纳摩尔级效力 (IC50：135-456 nM)，并能有效抑制 NF-κB 调节的 IL-6 和 I 型干扰素 (IFN-α) 反应，甚至抑制 IL-1β 和 IL-18 诱导的细胞因子[1]。
BMS-986126 对 MyD88 非依赖性激动剂 TLR3 和 TNF-α 诱导的细胞因子产生无显著影响[1]。
BMS-986126 (0-2 μM，30 分钟) 剂量依赖性地抑制人 PBMC 中 TLR2 和 TLR4 下游的 IKKα/β 和 ERK 以及 TLR7 下游的 ERK 的磷酸化[1]。
BMS-986126 在抑制健康供体和系统性红斑狼疮患者 PBMC 中 TLR7/9 诱导的干扰素反应基因表达 (例如 IFIT1) 方面表现出同等效力[1]。
BMS-986126 (5 μM，30 分钟) 可广泛逆转人 PBMC 中 TLR7 激活诱导的基因表达谱，其中相当一部分被抑制的基因是经典的干扰素刺激基因[1]。
BMS-986126 (16-80 nM，30 分钟) 与 Prednisolone (HY-17463) 联用可协同抑制人 PBMC 中 TLR9 诱导和流感病毒诱导的 IFIT1 表达，其抑制作用显著强于单药[1]。

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

BMS-986126 相关抗体:

Western Blot Analysis[1]

Cell Line: PBMCs
Concentration: 0, 0.07, 0.22, 0.67, 2 μM
Incubation Time: 30 min
Result: Inhibited LPS-induced IKKα/b and ERK phosphorylation. Inhibited TLR2-induced IKKα/b and ERK phosphorylation. Robustly inhibit Gardiquimod (HY-103697)-induced ERK phosphorylation
体内研究
(In Vivo)

BMS-986126 (0.1-3 mg/kg，口服，单次给药，在 LTA/CpG-ODN/Gardiquimod 前 30 分钟给药) 可抑制小鼠体内多种MyD88依赖性 TLR (TLR2/7/9) 下游的细胞因子生成[1]。
BMS-986126 (0.3-10 mg/kg，口服，每日一次，持续 6 天或 8 周) 可显著抑制自发性 (MRL/lpr 和 NZB/NZW) 小鼠狼疮模型中的疾病活动[1]。

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

Animal Model: Female BALB/c mice intraperitoneally injected with LTA (25 mg/kg)[1]
Dosage: 0.1, 0.3, 1.0, and 3.0 mg/kg
Administration: p.o., single dose 30 min pre-LTA
Result: Dose-dependently suppressed LTA-induced IL-6 plasma levels, with maximal inhibition observed at the top dose of 3 mg/kg.
Animal Model: Male C57BL/6 mice (12-week-old) intravenously injected with CpG-ODN (2.5 μg)[1]
Dosage: 1 and 3 mg/kg
Administration: p.o., single dose 30 min pre-CpG-ODN
Result: Strongly suppressed IFN-α at both 2 and 8 h after CpG-ODN challenge.
No IFN-α was detected in any group at 24 h after CpG-ODN challenge.
Animal Model: Male C57BL/6 mice (12-week-old) intraperitoneally injected with Gardiquimod (5 mg/kg)[1]
Dosage: 1 and 3 mg/kg
Administration: p.o., single dose 30 min pre-Gardiquimod
Result: Dose-dependently suppressed both IFN-α and IL-6 production at both 2 and 8 h after Gardiquimod challenge.
Animal Model: Male MRL/lpr mice (12-14 weeks old)[1]
Dosage: 0.3, 1, 3, and 10 mg/kg
Administration: p.o., daily for 8 weeks
Result: Dose-dependently suppressed biomarkers of kidney damage and systemic inflammation.
Showed very strong inhibition of kidney damage end points, including reduction of absolute protein levels in the urine, urine NGAL levels, and serum blood urea nitrogen.
Demonstrated significant protection of all end points at 1 mg/kg.
Dose-dependently suppressed dsDNA-specific autoantibody titers, as well as plasma levels of IL-10 and IL-12p40.
Significantly suppressed the percentage of splenic IFN-α+ pDCs at both the 1 and 10 mg/kg doses.
Suppressed IL-6 production by splenic CD11b+ myeloid cells.
All but the lowest dose inhibited IgG deposition in the kidney.
Dose-dependently suppressed histopathology in the kidney.
Animal Model: Male C57BL/6 mice induced by Imiquimod (HY-B0180)[1]
Dosage: 0.3, 1, 3, and 10 mg/kg
Administration: p.o., daily for 6 days
Result: Dose-dependently suppressed skin thickening, scaling, erythema, and spleen weight gain.
Significantly inhibited skin histopathology at 3 and 10 mg/kg.
Maintained its plasma levels above the mouse in vitro whole blood LTA-induced IL-6 IC50 value for 24 h.
Maintained its concentrations above the mouse whole blood IC50 value (LTA-induced IL-6 IC50) for 8-12 h out of the day.
Animal Model: Female NZB/NZW mice (12-14 weeks old)[1]
Dosage: 0.3, 1, 3, and 10 mg/kg
Administration: p.o., daily for 25 weeks
Result: Strongly suppressed biomarkers of kidney damage at all doses tested, including urine protein levels and urine levels of NGAL.
Dose-dependently suppressed systemic end points including dsDNA-specific autoantibody titers and plasma IL-12p40 levels.
Inhibited the percentage of splenic IFN-α+ pDCs.
Significantly inhibited the expression of the IFN response gene IFIT1 in peripheral blood.
Dose-dependently inhibited IgG deposition in the kidney.
Significantly suppressed histopathology in the kidneys with profound effects on glomerular damage and tubular damage subscores.
分子量

424.47

Formula

C22H25FN6O2
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

BMS-986126 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

BMS-9861261610017-20-3BMS986126BMS 986126IRAKToll-like Receptor (TLR)ERKNF-κBInterleukin RelatedInterleukin-1 receptor associated kinaseIL-1R associated kinaseExtracellular signal regulated kinasesNuclear factor-κBNuclear factor-kappaBILIRAK4MyD88-dependentMRL/lprNZB/NZWSLETLRIFN-αIL-6Inhibitorinhibitorinhibit

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