R406
Catalog No.S2194
Molecular Weight(MW): 628.63
R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.
6 Customer Reviews
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Platelets (3 x 108/mL) were preincubated with Y27632 (10 uM), R406 (1 uM), or a combination of Y27632 and R406 for 20 minutes followed by stimulation with oxLDL (50 ug/mL) for 15 seconds and lysis. Samples were then separated by SDS-PAGE and were immunoblotted for phospho-MLCSer19, followed by reprobing for β-tubulin. (Fi) Representative blots. (Fii) Densitometric analysis of 3 independent experiments. *P < .05. Data are presented as mean ± SEM. Experiments were carried out in the presence of apyrase (2 U/mL), indomethacin (10 uM), and EGTA (1 mM).
Blood 2014 122(4), 580-9. R406 purchased from Selleck.
The patient's CLL cells were exposed to dabrafenib, vemurafenib, R406, or DMSO as control at the indicated concentrations, and the resulting Western blot and the RAS-GTP/tRAS ratios are shown. One of 3 independent experiments with similar results is shown.
J Clin Invest 2014 124(11), 5074-84. R406 purchased from Selleck.
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(C) Z-138 and JEKO-1 cells were simultaneously exposed to sorafenib and R406 at the indicated doses, and cell viability was determined at 48 hours by annexin V/PI staining. Bars represent the mean ± SD of 3 independent experiments. CI value is indicated for each combination. (D) Primary MCL cells from 7 patients were simultaneously exposed to sorafenib and R406 at the indicated doses for 48 hours, and cell viability was determined as above. Bars represent the mean ± SEM of all the samples analyzed. CI value is indicated for each combination.
Clin Cancer Res 2013 19, 586-597. R406 purchased from Selleck.
NHEKs were treated with R406 (1 μM) for 1, 3, and 5 days. Then cells were collected for the protein analysis by Western blot.
J Invest Dermatol, 2016, 136(1):192-201. R406 purchased from Selleck.
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(M-CSF)-M2 macrophages were exposed to M860-IC (30 µg/ml) for 18 h in the presence of heparin or R406 (0, 1, 3 µM), mAbs against human CD14, CD16, CD32, CD64, or CLI-095 (5 µM). Isotype-matched irrelevant Abs as well as untreated (M-CSF)-M2 cells (M) were included as controls. TNFα in the culture supernatant was quantitated using ELISAs.
Front Immunol, 2018, 9: 37. R406 purchased from Selleck.
Neutrophils were pretreated or untreated with the indicated concentrations of R406 for 1 hr. The cells were stimulated with SAA (5 ug/ml) for 4 hr. The cells were harvested and analyzed for NLRP3 mRNA by RT-PCR. Three experiments were performed using different neutrophils and a representative result is shown.
PLoS One 2014 9(5), e96703. R406 purchased from Selleck.
Purity & Quality Control
Choose Selective Syk Inhibitors
Biological Activity
| Description | R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Features | Lead drug candidate for rheumatoid arthritis. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
R406 is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling. R406 inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. R406 inhibits phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 binds to the ATP binding pocket of Syk and inhibits its kinase activity as an ATP-competitive inhibitor with Ki of 30 nM. R406 blocks Syk-dependent FcR-mediated activation of monocytes/macrophages and neutrophils and Bcr-mediated activation of B lymphocytes. [1] R406 significantly induces chronic lymphocytic leukemia (CLL) cell apoptosis in nurselike cells cocultures and blocks CCL3 and CCL4 secretion by CLL cells in response to B-cell antigen receptor (Bcr) triggering. [2] R406 is a potent inhibitor of platelet signaling and functions initiated by FcγRIIA cross-linking by specific antibodies or by sera from HIT patients. [3] |
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| Cell Data |
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| In vivo | R406 reduces cutaneous reverse passive Arthus reaction by approximately 86% at 5 mg/kg in prophylactic treated mice. R406 also shows efficacy in inhibiting paw inflammation in antibody-induced arthritis mouse models. [1] R406 does not adversely affect macrophage or neutrophil function in innate immune responses and has minimal functional immunotoxicity notwithstanding its lymphocytopenic effect. [4] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (159.07 mM) |
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| Water | Insoluble | |
| Ethanol | 0 mg/mL (0.0 mM) | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%dmso+95%cornoil For best results, use promptly after mixing. |
6mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 628.63 |
|---|---|
| Formula | C22H23FN6O5.C6H6O3S |
| CAS No. | 841290-81-1 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
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Question 1:
What’s the difference between S1533 and S2194?
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Answer:
S1533 and S2194 are two different forms of R406. S1533 is the free base form, containing only R406 molecule without a acid added to it. S2194 has an additional C6H6O3S acid on it which makes the molecule a salt form. The free base and salt forms have same biology activities. Free base has a lower molecular weight and salt form has a better solubility in DMSO.
