428205-M

Lck Inhibitor

The Lck Inhibitor, also referenced under CAS 213743-31-8, controls the biological activity of Lck. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 別名: Lck Inhibitor, 4-Amino-5-(4-phenoxyphenyl)-7H-pyrrolo[3,2-d]pyrimidin-7-yl-cyclopentane
• 実験式（ヒル表記法）: C₂₃H₂₂N₄O
• CAS番号: 213743-31-8
• 分子量: 370.45
• MDL番号: MFCD04974490
• UNSPSCコード: 12352200

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 17 mg/mL
• 保管温度: 2-8°C
• SMILES記法: [n]2(c3ncnc(c3c(c2)c4ccc(cc4)Oc5ccccc5)N)C1CCCC1
• InChI: 1S/C23H22N4O/c24-22-21-20(14-27(17-6-4-5-7-17)23(21)26-15-25-22)16-10-12-19(13-11-16)28-18-8-2-1-3-9-18/h1-3,8-15,17H,4-7H2,(H2,24,25,26)
• InChI Key: FMETVQKSDIOGPX-UHFFFAOYSA-N

詳細

詳細

A cell-permeable pyrrolopyrimidine compound that acts as a potent, reversible, selective, and ATP-competitive inhibitor of Lck (IC₅₀ at 5 µM ATP = <1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck_64-509 Y³⁹⁴, Lckcd pY³⁹⁴, Src, Kdr and Tie-2, respectively; IC₅₀ at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck_64-509 Y³⁹⁴, Blk, Fyn, Lyn and Csk, respectively). Only minimally affects the activities of other kinases (IC₅₀ = 3.2 µM, >33 µM, >50 µM and >50 µM for EGFR, PKC, CDC2/B and ZAP-70, respectively). Also shown to potently block T-cell receptor-stimulated IL-2 production in vitro (IC₅₀<1-40 nM in Jurkat T cells) and in vivo (ED₅₀ = 4 mg/kg in mice, ip.)

生物化学的／生理学的作用

Primary Target
Lck₆₄₋₅₀₉ Y³⁹⁴

Target IC₅₀: At5 µM ATP = <1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for lck64-509 Y394, Lckcd pY394, Src, Kdr and Tie-2, respectively; IC50 at 1 mM ATP = 16 µM, 66 nM, 126 nM, 420 nM and 5.18 µM for Lck64-509 Y394, Blk, Fyn, Lyn and Csk

警告

Toxicity: Harmful (C)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

その他情報

Burchat, A.F., et al. 2000. Bioorg. Med. Chem. Lett.10, 2171.
Arnold. L.D., et al. 2000. Bioorg. Med. Chem. Lett.10, 2167.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3