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20

抑制剂 & 化合物

16

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16526	Phorbol 12,13-dibutyrate PDBu,Phorbol dibutyrate	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	Phorbol 12,13-dibutyrate is a PKC activator. It also is a potent skin tumor promoter.
T26386	4alpha-PDD 4α-Phorbol 12,13-didecanoate
	4alpha-PDD activates transient receptor potential vanilloid 4 (TRPV4) channels and is inactive for signaling through PKC.
T36696	DMBA
	7,12-Dimethylbenz[a]anthracene (DMBA) is a polycyclic aromatic hydrocarbon (PAH) that has been found in tobacco smoke and diesel exhaust and has carcinogenic activity.1,2It undergoes metabolic activation by numerous enzymes, including the cytochrome P450 (CYP450) isoform CYP1B1, as well as microsomal epoxide hydrolase (mEH), producing a variety of reactive metabolites that form DNA adductsin vivo, and it has been commonly used to induce tumor formation in various rodent models.2,3,1DMBA increase...
T68654	Sapintoxin D
	Sapintoxin D is a fluorescent phorbol ester and selective activator of protein kinase C.
T28975	Tigilanol tiglate EBC-46,EBC 46,EBC46
	Tigilanol tiglate is a phorbol ester and acts as a protein kinase C regulator along with other related compounds.
T36412	Multiflorenol
	Multiflorenol is a triterpene that has been found in T. kirilowii seeds.1 It inhibits in vitro activation of Epstein-Barr virus early antigen (EBV-EA) induced by the tumor promoter phorbol 12-myristate 13-acetate in a concentration-dependent manner. \|1. Akihisa, T., Tokuda, H., Ichiishi, E., et al. Anti-tumor promoting effects of multiflorane-type triterpenoids and cytotoxic activity of karounidiol against human cancer cell lines. Cancer Lett. 173(1), 9-14 (2001).
T37278	2-chloro Stearic Acid
	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).
T37983	GM 1489
	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 phor...
T37321	RN-9893 (hydrochloride)
	RN-9893 is an antagonist of transient receptor potential vanilloid 4 (TRPV4; IC50s = 0.42 and 0.66 μM, respectively, for the human and rat receptors).1 It is selective for TRPV4 over TRPV1, TRPV3, and TRPM8 (IC50s = 10, >30, and 30 μM, respectively). RN-9893 reduces rat TRPV4 activity induced by 4α-phorbol 12,13-didecanoate or hypotonicity (IC50s = 0.57 and 2.1 μM, respectively, in cell free assays). \|1. Wei, Z.L., Nguyen, M.T., O'Mahony, D.J., et al. Identification of orally-bioavailable antago...
T36320	C6 L-threo Ceramide (d18:1/6:0) C6 L-threo Ceramide (d18:1/6:0)
	C6 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 L-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 L-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 L-threo Ceramide enhances IL-4 production induced by phorbol 12-myristate 13-acetate in EL4 T cells when used at a concentration of 10 μM.
T69244	Betulonaldehyde
	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 t...
T37564	C4 Ceramide (d18:1/4:0) C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)
	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...
T36221	2-chloro Palmitic Acid
	2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endot...
T37565	C6 D-threo Ceramide (d18:1/6:0) C6 D-threo Ceramide (d18:1/6:0)
	C6 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides., C6 D-threo Ceramide is cytotoxic to U937 cells in vitro (IC50 = 18 μM). It is metabolically inactive and, unlike C6 L-erythro ceramide , C6 D-threo ceramide cannot be converted to C6 glucosylceramide by ceramide glucosyltransferase. C6 D-threo Ceramide promotes survival of isolated rat spinal neurons when used at concentrations up to 2.5 μM but induces cell death at concentrations greater...
T35927	C2 L-threo Ceramide (d18:1/2:0) C2 L-threo Ceramide (d18:1/2:0)
	C2 L-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide . C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1...
T37439	C18 Globotriaosylceramide (d18:1/18:0)
	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 lysosoma...
T83728	Tat-AKAP79 (326-336) TFA Tat-A-kinase Anchor Protein 79 (326-336)
	Tat-AKAP79 (326-336) 是一种肽，由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下，能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内，Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期，并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。
T81451	PKCd (8-17)
	PKCd (8-17) 是源自蛋白激酶 C (PKC)d V1 结构域的生物活性肽。它能抑制由佛波醇 12-肉豆蔻酸酯 13-乙酸酯 (PMA) 诱导的 PKCd 易位和激活。此外，PKCd (8-17) 在降低心脏和脑细胞缺血损伤、促进成纤维细胞增殖、以及抑制小鼠移植冠状动脉疾病方面具有潜在应用。
T36235	5-Chlorouracil
	5-Chlorouracil is a chlorinated derivative of the pyrimidine nucleoside base uracil . In vivo, it is converted into chlorodeoxyuridine, which is mutagenic and genotoxic.1 Uracil is chlorinated at the 5 position in a cell-free myeloperoxidase, peroxide, and chloride system in which hypochlorous acid is formed.2 5-Chlorouracil has been found in human neutrophils stimulated with phorbol 12-myristate 13-acetate in vitro and in inflammatory human exudate isolated from sites of superficial infection. ...
T83701	TRPV1-Tat TFA Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat
	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。

化合物

Phorbol 12,13-dibutyrate

Cat.No: T16526

Synonym: PDBu,Phorbol dibutyrate

Target: PKC

Cat.No: T26386

Synonym: 4α-Phorbol 12,13-didecanoate

Cat.No: T36696

Cat.No: T68654

Tigilanol tiglate

Cat.No: T28975

Synonym: EBC-46,EBC 46,EBC46

Cat.No: T36412

2-chloro Stearic Acid

Cat.No: T37278

Cat.No: T37983

RN-9893 (hydrochloride)

Cat.No: T37321

C6 L-threo Ceramide (d18:1/6:0)

Cat.No: T36320

Synonym: C6 L-threo Ceramide (d18:1/6:0)

Betulonaldehyde

Cat.No: T69244

C4 Ceramide (d18:1/4:0)

Cat.No: T37564

Synonym: C4 Ceramide (d18:1/4:0),Cer(d18:1/4:0)

2-chloro Palmitic Acid

Cat.No: T36221

C6 D-threo Ceramide (d18:1/6:0)

Cat.No: T37565

Synonym: C6 D-threo Ceramide (d18:1/6:0)

C2 L-threo Ceramide (d18:1/2:0)

Cat.No: T35927

Synonym: C2 L-threo Ceramide (d18:1/2:0)

C18 Globotriaosylceramide (d18:1/18:0)

Cat.No: T37439

Tat-AKAP79 (326-336) TFA

Cat.No: T83728

Synonym: Tat-A-kinase Anchor Protein 79 (326-336)

Cat.No: T81451

Cat.No: T36235

Cat.No: T83701

Synonym: Transient Receptor Potential Vanilloid 1-Tat,736-745-Tat

Cat. No.	Product Name	Target	Signaling Pathways
T4037	Phorbol 4β-Phorbol,佛波醇,(+)-Phorbol	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	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。
TQ0198	Phorbol 12-myristate 13-acetate 佛波醇12-十四酸酯13-乙酸酯,PMA	NF-κB; S1P Receptor; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; NF-κB
	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。
TN4768	Phorbol 13-acetate	Others	Others
	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。
T81484	Phorbol 12-tiglate
	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。
T72533	4-Deoxy-4α-phorbol
	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。
T83526	(Rac)-Phorbol-12-(2-methylbutyrate)
	(Rac)-Phorbol-12-(2-methylbutyrate)为从巴豆油中分离所得的天然化合物。
T22471	12-O-Tiglylphorbol-13 –isobutyrate	Others	Others
	The compound is extracted from Croton tiglium dried fruit.
TN1441	Beta-Tocopherol β-生育酚,BETA-生育酚	ERK; MAPK	MAPK
	Beta-Tocopherol 对由 phorbol 12-myristate 13-acetate (PMA) 诱导的人红白血病细胞 (HEL) 粘附有影响。
TN1110	Shanziside 山栀苷,Shanzhiside	IL Receptor	Immunology/Inflammation
	Shanziside (Shanzhiside) 是一种分离自福洛美属植物中的环烯醚萜苷类化合物。
T3889	Platycodin D	Prostaglandin Receptor; AMPK	Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; PI3K/Akt/mTOR signaling
	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。
TN1227	25R-Inokosterone	TNF	Apoptosis
	25S-Inokosterone and 25R-inokosterone exhibit potent inhibition (80-95% at ) against TNF-expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells, they have excellent anti-atopy activity, thus they could be used to a large range of
TN5852	Oleuropeic acid
	(+)-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.
TN1228	25S-Inokosterone	TNF	Apoptosis
	25S-Inokosterone and 25R-inokosterone exhibit potent inhibition (80-95% at ) against TNF-expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells, they have excellent anti-atopy activity, thus they could be used to a large range of
T38262	Sphingosine (d14:1)
	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).
T35741	Gliovirin
	Gliovirin is a fungal metabolite that has been found inT. harzianumand has fungicidal, antimicrobial and anti-inflammatory activities.1It is active against the plant pathogenic fungusP. ultimum(MIC = 60 ng/ml) and the parasiteT. brucei brucei(IC50= 90 ng/ml), but has no effect on the plant pathogenic fungiR. solani,P. omnivorum,T. basicola,R. arrhizus, andV. dahliaeor the bacteriaB. thuringiensis,P. fluorescens, andX. malvacearumwhen used at concentrations up to 1,000 ng/ml.2,3Gliovirin decrease...
T37291	Lyso-Globotriaosylceramide (d18:1) Lyso-Globotriaosylceramide (d18:1)
	Lyso-globotriaosylceramide is a form of globotriaosylceramide that is lacking the fatty acyl group. It binds to Shiga toxin 1 (Stx1) in the presence of cholesterol and phosphatidylcholine but does not bind Stx2. It also reduces viability and aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate when used at concentrations of 50 and 1 μM, respectively. Lyso-globotriaosylceramide accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry diseas...

天然产物

Cat.No: T4037

Synonym: 4β-Phorbol,佛波醇,(+)-Phorbol

Target: PKC

Phorbol 12-myristate 13-acetate

Cat.No: TQ0198

Synonym: 佛波醇12-十四酸酯13-乙酸酯,PMA

Target: NF-κB, S1P Receptor, PKC

Phorbol 13-acetate

Cat.No: TN4768

Target: Others

Phorbol 12-tiglate

Cat.No: T81484

4-Deoxy-4α-phorbol

Cat.No: T72533

(Rac)-Phorbol-12-(2-methylbutyrate)

Cat.No: T83526

12-O-Tiglylphorbol-13 –isobutyrate

Cat.No: T22471

Target: Others

Beta-Tocopherol

Cat.No: TN1441

Synonym: β-生育酚,BETA-生育酚

Target: ERK, MAPK

Cat.No: TN1110

Synonym: 山栀苷,Shanzhiside

Target: IL Receptor

Cat.No: T3889

Target: Prostaglandin Receptor, AMPK

25R-Inokosterone

Cat.No: TN1227

Target: TNF

Oleuropeic acid

Cat.No: TN5852

25S-Inokosterone

Cat.No: TN1228

Target: TNF

Sphingosine (d14:1)

Cat.No: T38262

Cat.No: T35741

Lyso-Globotriaosylceramide (d18:1)

Cat.No: T37291

Synonym: Lyso-Globotriaosylceramide (d18:1)

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