2. Cell Cycle/DNA Damage Immunology/Inflammation
  3. CDK Interleukin Related
  4. RO8323

RO8323 是一种具有口服活性的、选择性的 CDK8/CDK19 抑制剂，对 CDK8 的 IC50 为 2 nM，对 CDK19 的 IC50 为 3 nM。RO8323 可促进调节性 T 细胞分化，抑制效应 T 细胞生成，逆转 Teff/Treg 比值，上调髓样细胞中 IL-10 的产生，并抑制 TNF-α、IL-6 和 IL-12 的产生。RO8323 可增强免疫重建，并呈剂量依赖性延长心脏移植物存活时间。RO8323 可用于慢性移植物抗宿主病、心脏移植物排斥反应、急性移植物抗宿主病及实验性自身免疫性脑脊髓炎的研究。

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RO8323

RO8323 Chemical Structure

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RO8323 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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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 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO8323 is an orally active, selective CDK8/CDK19 inhibitor, with an IC50 of 2 nM against CDK8 and 3 nM against CDK19. RO8323 promotes regulatory T cell differentiation, inhibits effector T cell generation, reverses the Teff/Treg ratio, upregulates IL-10 production in myeloid cells, and suppresses the production of TNF-α, IL-6 and IL-12. RO8323 enhances immune reconstitution and prolongs cardiac allograft survival in a dose-dependent manner. RO8323 can be used in the research of chronic graft-versus-host disease, cardiac allograft rejection, acute graft-versus-host disease and experimental autoimmune encephalomyelitis[1].

IC50 & Target[1]

CDK8

2 nM (IC50)

CDK19

3 nM (IC50)

IL-10

 

IL-6

 

IL-12

 

体外研究
(In Vitro)

RO8323 可强效且选择性地抑制纯化的 CDK8 (IC50 = 2 nM) 和 CDK19 (IC50 = 3 nM) 酶，对激酶组的选择性超过 100 倍[1]。
RO8323 (0.01-1 μM; 4 天) 可呈剂量依赖性地增强小鼠初始 CD4+T 细胞中 CD25+Foxp3+调节性 T 细胞 (Treg) 的分化，在 1 μM 作用 4 天后分化水平较对照提升 1.3 倍，同时上调 Treg 的功能标志物[1]。
RO8323 (0.01-1 μM; 6 天) 可剂量依赖性地促进 hCD4+ T 细胞中 CD25+Foxp3+调节性 T 细胞 (Treg) 的分化，在 1 μM 作用 6 天后分化水平较对照提升 1.6 倍，同时上调 Treg 的功能标志物[1]。
RO8323 (0.01-1 μM; 18 h) 可呈剂量依赖性地增强经 R848 刺激的单核细胞来源树突状细胞中 IL-10 的产生，并抑制促炎细胞因子 (TNF-α、IL-6、IL-12) 的表达[1]。

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

RO8323 相关抗体:
体内研究
(In Vivo)

RO8323 (3 mg·kg-1·d-1；灌胃；每日；移植后第 7 天至第 49 天) 可在小鼠慢性移植物抗宿主病 (cGVHD) 模型中实现 100% 的存活率，减轻肾脏病理损伤，抑制炎症介质，并恢复多谱系免疫重建[1]。
RO8323 (3-10 mg·kg-1·d-1；灌胃；每日；移植后第 0 天至第 20 天) 可在小鼠模型中剂量依赖性地延长心脏移植物存活时间，其中 10 mg·kg-1·d-1 剂量组的存活率达 90%，同时伴随调节性 T 细胞 (Treg) 的持续性扩增[1]。
RO8323 (10 mg·kg-1·d-1；灌胃；每日；诱导后第 0 天) 可完全阻止小鼠 MOG 诱导的 EAE 模型的疾病发作，使外周 Treg 频率升高 1.7 倍，并抑制致病性 Th1 和 Th17 细胞群[1]。
RO8323 (1-30 mg·kg-1；灌胃；单次；LPS 攻击前 30 分钟) 可呈剂量依赖性升高 LPS 攻击小鼠的血清 IL-10 水平[1]。

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

Animal Model: BALB/c (male, 7-9 weeks old, cGVHD model via sublethal 6.5 Gy irradiation + intravenous transfer of 5×106 T cell-depleted bone marrow cells plus 40×106 CD25-depleted splenocytes from allogeneic DBA/2 donors)[1]
Dosage: 3 mg·kg-1·d-1
Administration: i.g.; daily; day 7 to day 49 post-transplantation
Result: Achieved 100% survival (vs. 36% in allogeneic vehicle controls).
Reduced proteinuria, as shown by lower area under the curve values and reduced peak proteinuria levels.
Reversed glomerulosclerosis and mesangial matrix lesions, resulting in significantly lower renal histopathology scores.
Suppressed renal inflammatory mediators BAFF, MCP-1, and CXCL10 by 68%, 69%, and 75% respectively.
Showed a non-significant increasing trend in peripheral CD25+Foxp3+ Treg frequencies.
Uniquely restored multi-lineage immune reconstitution (CD45+ leukocytes, CD4+ T cells, CD8+ T cells, B cells, monocytes, NK cells) compared to allogeneic vehicle controls.
Animal Model: C3H/HeN (male, 6-8 weeks old, cardiac allograft rejection model via neonatal BALB/c mouse hearts implanted into ear pinnas)[1]
Dosage: 3 mg·kg-1·d-1; 10 mg·kg-1·d-1
Administration: i.g.; daily; day 0 to day 20 post-transplantation
Result: Dose-dependently prolonged cardiac allograft survival, with 50% graft survival at the 3 mg·kg-1·d-1 dose and 90% graft survival at the 10 mg·kg-1·d-1 dose at day 20 post-transplantation (vs. 20% in untreated allograft controls).
Increased peripheral CD25+Foxp3+ Treg frequencies to 2-fold at the 10 mg·kg-1·d-1 dose by day 10 post-transplantation, with effects persisting to day 20 (3-fold increase).
分子量

315.37

Formula

C19H17N5
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

RO8323 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:

RO8323RO 8323RO-8323CDKInterleukin RelatedCyclin dependent kinaseILIL-6effector T cellchronic graft-versus-host diseasecardiac allograft rejectionCDK8IL-10TNF-αregulatory T cellIL-12CDK19Inhibitorinhibitorinhibit

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目录号：
HY-183074
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