PADI4_11
PADI4_11 is an isoform-selective, allosteric PADI4 activator with a Kd of 457 nM. PADI4_11 enters cells via active transport, does not induce cytotoxicity or membrane damage, and serves as a tool for investigating the regulation, function and cellular reprogramming of PADI4. PADI4_11 can be used in studies related to rheumatoid arthritis and ulcerative colitis.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C70H109N21O20S
- 分子量:1596.81
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
PADI4_11 binds selectively to calcium-bound and active-site-blocked calcium-bound recombinant hPADI4 with nanomolar affinity, but does not bind to calcium-free PADI4[1].
PADI4_11 (0.003-100 μM) allosterically activates recombinant PADI4 by reducing its calcium ion requirement, enhances the maximum activity under calcium ion-saturated conditions, and exhibits isozyme selectivity for PADI4[1].
PADI4_11 (100 nM-50 μM; 4 h) exhibits cell permeability in HaLo-GFP-mito HeLa cells, and its uptake is partially mediated by active transport mechanisms[1].
PADI4_11 (1-50 μM; 1 h) specifically activates PADI4 in hPADI4-stable mouse embryonic stem cells (mES cells) without additional stimulation, shows no off-target effect on mouse PADI4, and exhibits no signs of cytotoxicity[1].
PADI4_11 specifically binds to recombinant PADI4 in the calcium-bound active conformation, even when the active site is blocked, with a Kd value of 457 nM for the calcium-bound form[2].
PADI4_11 (100 nM-50 μM; 4 h) exhibits cell permeability in HaLo-GFP-mito HeLa cells, with a CP50 value of 3.1 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:hPADI4-stable mouse embryonic stem (mES) cells, wild-type mES cells
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Concentration:1-50 μM
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Incubation Time:1 h
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Result:Induced dose-dependent increases in H3Cit intensity in hPADI4-stable mES cells, with an EC50 of 15.62 μM.
Showed no induction of H3Cit in wild-type mES cells (which only express mouse PADI4) at any tested concentration.
Did not increase intracellular calcium levels or cause cell membrane permeability/propidium iodide uptake at tested concentrations.
化学情報
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分子量 1596.81
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分子式 C70H109N21O20S
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配列
Ac-Tyr-Glu-Ser-Cys-Arg-Tyr-Arg-Gln-Val-Leu-Gln-Leu-NH2 (thioether bond:Tyr1-Cys4)
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シーケンスの短縮
Ac-YESCRYRQVLQL-NH2 (thioether bond:Tyr1-Cys4)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)