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

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.

For research use only. We do not sell to patients.

RKER-216

RKER-216 Chemical Structure

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RKER-216 Related Antibodies

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Description

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].

Species Reactivity

Human
IC50 & Target[1]

ACVR1

58.7 pM (Kd)

In Vitro

RKER-216 (0.02-1 μg/mL, 6 h) binds to ALK2 with a KD of 58.7 pM, but does not bind to ALK3 at a concentration 10-fold higher than those necessary to bind ALK2[1].
RKER-216 achieves potential interactions between ALK2 with a robust peptide coverage of 92.2% in ACVR1 knockout in HepG2 and Huh7 cells[1].
RKER-216 (0.02-30 μg/mL,6 h) inhibits alk2-mediated hepcidin transcription in Hep3B cells (0.02-1 μg/mL), HepG2 (ACVR1 knockout (KO)) (1-30 μg/mL) and Huh7 cell (ACVR1 knockout (KO)) (1-30 μg/mL) [1].

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

RKER-216 Related Antibodies

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.
In Vivo

RKER-216 (3 mg/kg, s.c. once ) inhibits ALK2 without impairing IL-6-mediated hepcidin induction but reduces overall hepcidin secretion via suppressing SMAD1/5/9 signaling in B6N mice[1].
RKER-216 (compound m216) (1-3 mg/kg, s.c., once, persisted for 6, 24 or 96 h) inhibited SMAD signaling to lower serum hepcidin, allowing more iron absorption to increase TSAT in TMPRSS6 KO mice[2].
RKER-216 (1 mg/kg, s.c., twice daily for 9 days) regulates iron metabolism through a unique mechanism that differs from intravenous iron in TMPRSS6 KO mice[2].
RKER-216 (1-3 mg/kg, s.c., twice daily for 3 weeks) g a dose proportional mitigation in improving microcytic anemia in TMPRSS6 KO mice[2].

MedChemExpress (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.
Gene ID

90  [NCBI]

Accession
Application

ELISA, FACS, Functional assay
Conjugated

Unconjugated
Reconsititution

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

Please refer to the lot-specific COA for specific buffer information.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RKER-216 Related Classifications

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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:

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

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