Calyculins are natural products originally isolated from the marine sponge Discodermia calyx.[2] . Calyculins have proven to be strong serine/threonine protein phosphatase inhibitors and based on this property, calyculins might be potential tumor-promoting agents. A laboratory synthesis of calyculin A has been reported. [3]

Calyculin A inhibits the activity of protein phosphatases PP1 and PP2A. Unlike Okadaic acid, which reduces PP2A activity but has little effect on PP1 activity, Calyculin A inhibits both …

花萼海绵体诱癌素A（Calyculin A，CAS NO：101932-71-2）最初是从海绵Disodermia calyx中分离到的一种海洋毒素，是一种具细胞渗透性、有效和选择性的蛋白磷酸酶1（PP1，IC50=0.3-0.7 nM）和蛋白磷酸酶2A（PP2A，IC50=0.5-1.0 nM）抑制剂。 对PP2B和PP2C的选择性＞10,000,000倍。 对酸性或碱性磷酸酶或磷酸-酪氨酸蛋白磷酸酶无抑制。 Calyculin A抑制平滑肌肌球蛋白B内源性磷酸酶的活性，诱导肌肉纤维收缩，并伴随细胞质游离Ca2+水平提高。 花 …

Calyculin A ( (-)-Calyculin A) 是有效，可渗透细胞的蛋白磷酸酶 1 (PP1) 和蛋白磷酸酶 2A (PP2A) 抑制剂，其 IC50 值分别为 2 nM 和 0.5-1 nM。

Calyculin A is a more potent phosphatase inhibitor than Okadaic acid (2). As shown by Western blot, treatment of cells with 100 nM Calyculin A for 30 minutes induces threonine phosphorylation, detected by Phospho-Threonine-Polyclonal Antibody #9381.

Calyculin A is an inhibitor of vimentin protein phosphatases, but this molecule can also inhibit other cellular phosphatases like the one affecting myosin light chain and thus alter acto-myosin contractility of the cell.

2023年2月11日 · Calyculin A 是丝氨酸-苏氨酸蛋白磷酸酶 (PP) PP1 和 PP2A 的天然细胞渗透性抑制剂（IC50 分别为 0.3-0.7 和 0.5-1 nM）。 它对 PP2B、PP2C 和 PP4 没有显着影响 .

Calyculin A, Discodermia calyx, Calyculin A, CAS 101932-71-2, is a cell-permeable inhibitor of protein phosphatase 2A (IC₅₀ = 0.5-1 nM) and protein phosphatase 1 (PP1; IC₅₀ = 2 nM).

2015年10月1日 · Calyculin A is a major cytotoxic compound isolated from the Japanese marine sponge Discodermia calyx. Its potent cytotoxicity is attributable to the specific inhibition of protein phosphatases 1 and 2A, as in the case of okadaic acid and the microcystins.