phorbol

Phorbol 13-acetate 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN4768，CAS号为 32752-29-7。

Phorbol (4β-Phorbol) 是具有毒性的二萜类化合物，其酯类具有强大的生物活性。

Phorbol 12,13-dibutyrate (Phorbol dibutyrate) 是一种 PKC 激活剂,以浓度依赖性方式抑制α1-肾上腺素受体介导的正性肌力作用,诱导的孤立兔血管平滑肌收缩。

4α-Phorbol 是 PKC 激活剂 12-myristate 13-acetate 的衍生物。能在离体小鼠骨髓成红细胞中诱导染色体损伤。

4-Deoxy-4α-phorbol 是在 E. desmondi 中发现的一种四环二萜类物质。4-Deoxy-4α-phorbol 可用于半合成 HIV-1诱导的 MT-4 细胞的细胞病理学效应抑制剂和 4α-山梨醇酯。

Phorbol12-tiglate为Phorbol衍生物，后者乃巴豆油水解产物，可激活蛋白激酶C，进而促进肿瘤发展。Phorbol及其衍生物在生物医学领域，广泛用于建立致癌模型研究。

(Rac)-Phorbol-12-(2-methylbutyrate)为从巴豆油中分离所得的天然化合物。

Phorbol 12-myristate 13-acetate (PMA) 属于佛波酯类天然产物，是一种 PKC、SphK、NF-κB 的激活剂。Phorbol 12-myristate 13-acetate 可诱导 THP1 细胞分化。

4alpha-PDD activates transient receptor potential vanilloid 4 (TRPV4) channels and is inactive for signaling through PKC.

The compound is extracted from Croton tiglium dried fruit.

12-Deoxyphorbol 13-palmitate，这是一种从Euphorbia fischeriana根部提取的抗肿瘤中药单体。该化合物能够调节细胞周期的关键调控分子（例如cyclin B、cyclin A和CDC2），从而诱导胃癌细胞的周期阻滞及细胞凋亡（apoptosis）。此外，12-Deoxyphorbol 13-palmitate通过作用于APOL2，能有效抑制APOL2–SERCA2–PERK–HES1的信号通路，进而减缓肝纤维化的进程。

ER272 is a natural PKC activator, inducing hippocampal neurogenesis.

Prostratin(12-Deoxyphorbol-13-acetate，13-O-乙酰基-12-脱氧佛波醇)是一种具有口服活性的蛋白激酶C（PKC）激活剂，Ki值为12.5 nM。作为一种NF-κB激活剂，Prostratin可激活T细胞中HIV基因的表达。Prostratin能抑制急性髓系白血病（AML）细胞系的生长，并增强阿糖胞苷诱导的AML细胞分化。此外，Prostratin诱导KRAS磷酸化并抑制KRAS突变的肿瘤生长。

Platycodin D 是从桔梗中分离得到的一种皂苷类天然产物，是AMPKα的激活剂，具有抗肥胖活性。它可刺激 TNF-α 合成或抑制 TNF-α mRNA 的降解。

2-chloro Stearic acid is a bioactive fatty acid that accumulates in primary human monocytes and neutrophils as well as murine neutrophils stimulated with phorbol 12-myristate 13-acetate . It induces DNA release from primary human neutrophils. 2-chloro Stearic acid is toxic to C. quinquefasciatus larvae (LC50 = <1 ppm).

TRPV1-Tat是一种针对瞬时受体电位范烤苷1 (TRPV1) 的肽类拮抗剂。它由来自TRPV1的A-激酶锚蛋白(AKAP)结合域的736-745个氨基酸以及来自HIV Tat的细胞穿透肽序列组成。TRPV1-Tat (200 µM) 能够在使用初级小鼠背根神经节的整细胞膜片钳技术中抑制由热或棕榈酸酯12-肉豆蔻酸13-醋酸酯(PMA014)引起的电流。当以10或30 µM剂量给药时，它能增加大鼠后爪机械痛阈。

GM 1489 is a broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. It reduces 5-aza-2'-deoxycytidine-induced increases in MMP-1, MMP-2, MMP-3, MMP-7, MMP-9, and MMP-14 expression as well as cell invasion in AsPC-1, BxPC-3, Hs766T, MiaPaCa2, and PANC-1 cancer cells. Topical administration of GM 1489 (100 μg) inhibits increases in ear thickness and epidermal hyperplasia induced by phorbol 12-myristate 13-acetate and phorbol dibutyrate (PdiBu) in mice.

(+)-Oleuropeic acid shows potent in vitro antitumor-promoting activity, it also suppresses an in vivo two-stage carcinogenesis induced with nitric oxide and 12-O-tetradecanoyl phorbol 13-acetate (TPA) on mouse skin.

Sphingosine (d16:1), an unconventional sphingolipid, is synthesized through enzymatic reactions starting with the condensation of myristoyl-CoA and serine by serine palmitoyltransferase long-chain base subunit 3 (SPTLC3), which shows a preference for myristoyl-CoA. This compound is found in minute quantities in its free form in human plasma and as a component of various plasma sphingolipids, such as sphingosine-1-phosphate, ceramides, sphingomyelins, and in brain cerebrosides, albeit at lower concentrations than the more common d18:1 sphingoid base. Sphingosine (d16:1) acts as an inhibitor of PKC in mixed micelle assays and diminishes superoxide production triggered by phorbol 12-myristate 13-acetate in isolated human neutrophils, as well as inhibiting the growth of CHO cells with IC50 values of 1 and 3.2 µM, respectively. Additionally, the concentration of sphingolipids containing sphingosine (d16:1) in the plasma is linked to the dietary consumption of saturated fatty acids and protein among ethnic Chinese populations.

C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. C18 globotriaosylceramide also accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease.

Sphingosine (d14:1) is a bioactive sphingolipid that has been found in B. mori (silkworm), P. clarkii (crayfish), and A. aurita (jellyfish) extracts. It increases the germination rate of N. rileyi, an entomopathogenic fungus, with an EC50 value of 10.2 nM. Sphingosine (d14:1) inhibits protein kinase C (PKC) in vitro (IC50 = 7.3 mol%) as well as superoxide generation induced by phorbol 12-myristate 13-acetate in neutrophils and reduces growth of CHO cells (IC50s = 19 and 8 μM, respectively).

C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7 Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis.[3]

Betulonaldehyde is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found in Betula. It is active against P. falciparum (IC50 = 3.36 µg ml) and cytotoxic to NCI H187 lung cancer cells and non-cancerous Vero cells (IC50s = 19.23 and 17.09 µg ml, respectively). Topical application of betulonaldehyde (1 mg ear) reduces ear edema induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) in mice. It has also been used a precursor in the semisynthesis of C-2 and C-28 betulonic aldehyde derivatives.

Sapintoxin D is a fluorescent phorbol ester and selective activator of protein kinase C.