Rendomab B4
Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research.
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Human
Rendomab B4 (0.15-100 nM; overnight-1 h) binds specifically and with high affinity (apparent Kd*=0.15 nM) to human endothelin B receptor expressed on CHO-ETB cells, and does not cross-react with rodent endothelin B receptor or human endothelin A receptor[1].
Rendomab B4 (10 nM; overnight) does not compete with endothelin-1 or endothelin-3 for binding to human endothelin B receptor on CHO-ETB cells, indicating distinct binding sites[1].
Rendomab B4 (1 μg/mL; 90 min) recognizes a discontinuous conformational epitope formed by two non-contiguous sequences in the N-terminal domain of human endothelin B receptor, spanning residues 28-38 and 70-77[1].
Rendomab B4 (0.14-10 nM; overnight) binds specifically to human endothelin B receptor expressed on multiple melanoma cell lines, with the highest affinity for UACC-257 cells (apparent Kd=0.14 nM), and does not bind to endothelin B receptor on non-cancerous HEK293T or HUVEC cells[1].
Rendomab B4 (150 nM; 2 h 30 min) potently inhibits endothelin-1 and endothelin-3-induced phospholipase C activation in UACC-257 melanoma cells, reducing activity by approximately 75%[1].
Rendomab B4 (150 nM; 2 h 5 min) does not inhibit endothelin-1 or endothelin-3-induced ERK1/2 phosphorylation in UACC-257 melanoma cells, demonstrating a biased inhibitory effect on endothelin B receptor signaling pathways[1].
Rendomab B4 (150 nM; 22 h) completely inhibits endothelin-1-induced migration of UACC-257 melanoma cells, without affecting baseline cell migration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:UACC-257 human mela
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Concentration:150 nM (Rendomab B4, pre-incubation); 50 nM ET-1 (stimulation)
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Incubation Time:2 h (37°C, pre-incubation); 20 h (37°C, stimulation)
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Result:Completely abolished ET-1-induced UACC-257 cell migration, with migration levels matching unstimulated cells.
Had no effect on baseline cell migration in the absence of ET-1.
ET-1 increased UACC-257 cell migration by 3-fold compared to unstimulated cells.
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Cell Line:UACC-257 human melanoma cells
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Concentration:150 nM (Rendomab B4, pre-incubation); 50 nM ET-1 (stimulation)
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Incubation Time:2 h (37°C, pre-incubation); 20 h (37°C, stimulation)
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Result:Completely abolished ET-1-induced UACC-257 cell migration, with migration levels matching unstimulated cells.
Had no effect on baseline cell migration in the absence of ET-1.
ET-1 increased UACC-257 cell migration by 3-fold compared to unstimulated cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:athymic nude mice (female, 10 weeks old)[2]
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Dosage:4 mg/kg
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Administration:i.p.; 2 doses (Day 47 and Day 80)
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Result:Showed no effect on melanoma xenograft tumor progression over 136 days.
Resulted in all mice being sacrificed on Day 108 due to significant ulceration or excessively large tumor volume, matching vehicle control outcome.
Caused no behavioral signs of toxicity or weight loss.
EDNRB/Endothelin R
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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SMILES
[Rendomab B4]
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Synonyms
Rendomab-B49
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Borrull A, et al. Rendomab B4, a monoclonal antibody that discriminates the human endothelin B receptor of melanoma cells and inhibits their migration. MAbs. 2016;8(7):1371-1385. [Content Brief]
[2]. Herbet A, et al. Targeting the activated allosteric conformation of the endothelin receptor B in melanoma with an antibody-drug conjugate: mechanisms and therapeutic efficacy. BJC Rep. 2025;3(1):3. Published 2025 Jan 20. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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