myosin ii

para-Nitroblebbistatin 是无细胞毒性、无荧光、光稳定、特异性的肌球蛋白 II (Myosin II) 抑制剂。para-Nitroblebbistatin 可用于肌球蛋白 II 在生理学、发育和细胞生物学中特殊作用的相关研究。

(-)-Blebbistatin ((S)-(-)-Blebbistatin) 是 blebbistatin 的 S 对映异构体。(-)-Blebbistatin 是一种肌球蛋白 II 抑制剂 (IC50=0.5-5 μM)，具有有效性和选择性。(-)-Blebbistatin 可以用于抑制心肌肌球蛋白、非肌肉肌球蛋白II和骨骼肌肌球蛋白。

Blebbistatin ((±)-Blebbistatin) 是一种非肌肉肌球蛋白 II(NMII)选择性和非肌肉肌球蛋白重链9（MYH9）特异性的抑制剂，可促进角膜内皮细胞 (CEC) 的定向迁移并加速伤口愈合，并保留了细胞连接的完整性和屏障功能。

BTS (N-Tosylbenzylamine) 是一种选择性骨骼肌肌球蛋白 II 亚片段 1 (S1) ATPase 活性抑制剂，可特异性抑制骨骼肌快速纤维的收缩。它对肌动蛋白和 Ca2+刺激的肌球蛋白 S1 ATPase 的 IC50值约为 5 µM。

MLCK inhibitor peptide 18 acetate(224579-74-2 free base) 是肌球蛋白轻链激酶的选择性竞争性抑制剂 (IC50 = 50 nM)。显示出比 CaM 激酶 II 高 4000 倍的选择性，并且不抑制 PKA。细胞可渗透。

(+)-Blebbistatin 是 (–)-Blebbistatin 的非活性对映异构体。 (–)-Blebbistatin 是一种选择性肌球蛋白 II ATPase 抑制剂。

A-3 hydrochloride 是一种细胞可渗透的、可逆的、ATP 竞争性非选择性拮抗剂。它抑制 PKA 、酪蛋白激酶 II 和肌球蛋白轻链激酶，Ki 值分别为4.3 µM、5.1 µM 和7.4 µM。它还抑制 PKC 和酪蛋白激酶 I 的活性，Ki 分别为 47 µM 和 80 µM。

(S)-nitro-Blebbistatin is a more stable form of (-)-blebbistatin , which is a selective cell-permeable inhibitor of non-muscle myosin II ATPases. (-)-Blebbistatin rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications. The addition of a nitro group stabilizes the molecule to circumvent its degradation by prolonged blue light exposure. (S)-nitro-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

JB061是一种非肌肉肌球蛋白II抑制剂，针对心肌肌球蛋白、骨骼肌肌球蛋白和平滑肌肌球蛋白II的IC50分别为4.4 μM、9.1 μM和>100 μM。其对ATP酶活性的抑制作用较弱（IC50>200 μM）。此外，JB061对COS-7细胞显示出细胞毒性，IC50值为39 μM。

JB062是一种针对非肌肉肌球蛋白(nonmusclemyosin)的抑制剂，其IC50值对骨骼肌肌球蛋白为1.6μM、心肌肌球蛋白为5.4μM，而对平滑肌肌球蛋白II大于100μM。此化合物对人类癌细胞显示出细胞毒性，对正常细胞则无此作用。JB062在肌肉痉挛、慢性肌肉骨骼疼痛及肥厚型心肌病研究中有潜在应用价值。

(R)-(+)-Blebbistatin O-Benzoate is a derivative of Blebbistatin. (R)-(+)-Blebbistatin is a 1-phenyl-2-pyrrolidinone derivative and a selective inhibitor of non-muscle myosin II. It blocks cell blebbing rapidly and reversibly and also disrupts directed cell migration and cytokinesis in vertebrate cell. (R)-(+)-Blebbistatin can also inhibit contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly. (R)-(+)-Blebbistatin is suitable as a negative control for (S)-(-)-Blebblastatin.

JB002为一种肌球蛋白 II 抑制剂，IC50值不大于10 μM。适用于研究肌肉痉挛、慢性肌肉骨骼疼痛及肥厚型心肌病。

(S)-3'-hydroxy-Blebbistatin is a more stable and less phototoxic derivative of (–)-blebbistatin, retaining the latter's properties as a selective, cell-permeable inhibitor of non-muscle myosin II ATPases. Unlike its predecessor, (S)-3'-hydroxy-Blebbistatin exhibits reduced fluorescence, improving its utility in live cell imaging applications by diminishing degradation into cytotoxic intermediates under blue light exposure (450-490 nm). It effectively inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across various species with IC50 values ranging from 0.5-5 µM and shows minimal inhibition against smooth muscle myosin with an IC50 of 80 µM. This compound plays a critical role in preventing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells, mirroring the active (–)-blebbistatin enantiomer in mechanism and efficacy.

(S)-3'-amino Blebbistatin, retaining the active stereochemistry of the less stable and more phototoxic (–)-blebbistatin, serves as a refined selective cell-permeable inhibitor of non-muscle myosin II ATPases. This compound efficaciously inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across several species with IC50s ranging from 0.5-5 µM, and exhibits minimal inhibition against smooth muscle myosin (IC50= 80 µM). Its primary functions include obstructing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. (S)-3'-amino Blebbistatin overcomes (–)-blebbistatin’s limitation of rapid degradation under blue light (450-490 nm) exposure, which generates cytotoxic intermediates, thus posing a challenge for fluorescent live cell imaging applications. The introduction of a 3’-amino group to its structure notably reduces fluorescence while maintaining (–)-blebbistatin’s activity, making it a superior alternative for research purposes.

Cucurbitacin I, cytotoxic triterpenoid sterols isolated from plants, elicits the formation of actin phospho-myosin II co-aggregates by stimulation of the RhoA ROCK pathway and inhibition of LIM-Kinase.

Selective competitive inhibitor of myosin light chain kinase (IC50 = 50 nM). Displays 4000-fold selectivity over CaM kinase II and does not inhibit PKA. Cell permeable.