2. TGF-beta/Smad
  3. TGF-β Receptor
  4. RKER-216

RKER-216 是一种靶向 ALK2 的人源单克隆 IgG 抗体抑制剂，其 KD 为 58.7 pM。RKER-216 可降低 Hep3B 细胞中的铁调素转录水平。RKER-216 通过与 BMP 配体竞争结合 ALK2 的胞外结构域，从而抑制 BMP-SMAD 信号通路。RKER-216 在体内通过抑制 SMAD 信号通路降低铁调素，促进铁吸收与利用。在炎症条件下，RKER-216 能有效动员组织铁。RKER-216 可用于炎症性贫血的相关研究。

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RKER-216

RKER-216 Chemical Structure

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RKER-216 相关抗体

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查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RKER-216 is a human monoclonal IgG antibody inhibitor targeting ALK2 with a KD of 58.7 pM. RKER-216 reduces hepcidin transcription in Hep3B.RKER-216 competes with BMP ligands for binding to the extracellular domain of ALK2, thereby inhibiting BMP-SMAD signal. RKER-216 mobilizes tissue iron effectively in inflammatory conditions. RKER-216 improves microcytic anemia in a dose-dependent manner by inhibiting SMAD signaling to reduce hepcidin and promote iron absorption and utilization in vivo. RKER-216 can be used for research on anemia of inflammation[1][2].

反应种属

Human
IC50 & Target[1]

ACVR1

58.7 pM (Kd)

体外研究
(In Vitro)

RKER-216 (compound m216) (0.02-1 μg/mL，6 小时) 以 58.7 pM 的 KD 值结合 ALK2，且在比结合 ALK2 所需浓度高 10 倍的条件下仍不结合 ALK3[1]。
RKER-216 在 HepG2 和 Huh7 细胞的 ACVR1 敲除模型中，以 92.2% 的高肽段覆盖率实现与 ALK2 的潜在相互作用[1]。
RKER-216 (0.02-30 μg/mL， 6小时) 在 Hep3B 细胞 (0.02-1 μg/mL)、HepG2 细胞 (ACVR1 敲除) 以及 Huh7 细胞 (ACVR1 敲除) 中，均能抑制 ALK2 介导的铁调素转录[1]。

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

RKER-216 相关抗体:

Real Time qPCR[1]

Cell Line: Hep3B, HepG2 (ACVR1 knockout (KO)), and Huh7 cell (ACVR1 knockout (KO)) cell lines
Concentration: 0.02, 0.2 and 1 μg/mL and 0, 1, 10 and 30 μg/mL
Incubation Time: 6 h
Result: Resulted HAMP mRNA a dose dependent decrease (0.02, 0.2 and 1 μg/mL) in Hep3B cells.
Exhibited the greatest suppression in BMP6-stimulated hepcidin expression, followed by BMP2/6 and BMP2 in Hep3B cells at 0-1 μg/mL.
Did not decreased HAMP mRNA at 1-30 μg/mL in HepG2 (ACVR1 knockout (KO)) and Huh7 (ACVR1 knockout (KO)) cell lines.
体内研究
(In Vivo)

RKER-216 (3 mg/kg，单次皮下注射) 可在 B6N 小鼠中抑制 ALK2，在不损害 IL-6 介导的铁调素诱导作用的同时通过抑制 SMAD1/5/9 信号通路降低整体铁调素分泌[1]。
RKER-216 (compound m216) (1-3 mg/kg，皮下注射，单次给药，药效持续 6、24 或 96 小时) 在 TMPRSS6 基因敲除小鼠中通过抑制 SMAD 信号通路降低血清铁调素，从而促进铁吸收并提高转铁蛋白饱和度[2]。
RKER-216 (1 mg/kg，皮下注射，每日两次，持续 9 天) 在 TMPRSS6 基因敲除小鼠中通过一种区别于静脉补铁的独特机制调节铁代谢[2]。
RKER-216 (1-3 mg/kg，皮下注射，每日两次，持续 3 周) 在改善 TMPRSS6 基因敲除小鼠的小细胞性贫血方面呈现出剂量相关的缓解效果[2]。

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

Animal Model: B6N male mice (7 weeks)[1]
Dosage: 3 mg/kg
Administration: s.c. once followed by LPS (1 mg/kg, i.p.)
Result: Induced Liver Il6 mRNA and decreased serum IL-6.
Resulted a greater fold-change ((11.7-fold for Hamp mRNA and 3.2-fold for serum hepcidin).
Inhibited SMAD1/5/9 phosphorylation regardless of inflammatory status.
Failed to impair LPS-mediated STAT3 phosphorylation, and the same LPS-induced effect was seen in isotype control groups in immunoblot analyses.
Animal Model: TMPRSS6 KO mice (8-11 weeks) [2]
Dosage: 1 or 3 mg/kg
Administration: s.c., once, persisted for 6, 24 or 96 h
Result: Decreased liver smAD1/5/9 phosphorylation, hepcidin (Hamp) mRNA, and serum hepcidin levels dosed with 1 or 3 mg/kg for 6 h.
Decreased serum hepcidin by 88% and increased TSAT by 4-fold at 1 or 3 mg/kg for 24 h.
Had sustained effects by 96 h at 3 mg/kg.
基因 ID

90  [NCBI]

Accession
应用

ELISA, FACS, Functional assay
偶联物

Unconjugated
复溶方法

The product can be reconstituted/diluted with sterile PBS or saline.
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

RKER-216 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:

RKER-216RKER216RKER 216TGF-β ReceptorTransforming growth factor beta receptorsIgGHep3Banemia of inflammationInhibitorinhibitorinhibit

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