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23

抑制剂 & 化合物

10

天然产物

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Cat. No. Product Name Target Signaling Pathways
T67858 STIMA-1

2-Vinylquinazolin-4-ol,p53 Activator VII

Others Others
STIMA-1 (2-Vinylquinazolin-4-ol) 是一种活性化合物,可以恢复 p63 的活性。STIMA-1 可以刺激角质形成细胞的增殖和分化。
T15410 GNF351

Aryl Hydrocarbon Receptor Immunology/Inflammation
GNF351 是芳烃受体 (AhR) 的完全拮抗剂,具有抑制 DRE 依赖性和非依赖性活性的能力。它与结合到 AhR 的光亲和性 AhR 配体竞争,IC50为 62 nM。它在小鼠或人角质形成细胞中的毒性极小。
T76924 Efalizumab

Hu1124,HU 1124

Integrin Cytoskeletal Signaling
Efalizumab 是一种新型针对 T 细胞的有效调节剂,是人源化 LFA-1 α 亚基(CD11a)单克隆抗体。Efalizumab 对 T 细胞激活、皮肤T细胞运输和T细胞粘附到角质形成细胞有抑制作用,可用于研究斑块银屑病和银屑病关节炎。
TP1293 Jagged-1 (188-204) TFA(219127-21-6 free base)

Jagged-1 (188-204) TFA

Gamma-secretase Neuroscience; Proteases/Proteasome; Stem Cells
Jagged-1 (188-204) TFA(219127-21-6 free base) 是 JAG-1 蛋白的一个片段。 JAG-1 是 Notch 配体,是一种在皮肤中表达最明显的肽。 JAG-1 诱导表皮成熟。将淹没的角质形成细胞单层暴露于钙浓度升高的 JAG-1 会产生具有 loricrin 表达和 NF-alphaB 激活的分层。
T77677 12R-LOX-IN-2

Lipoxygenase Metabolism
12R-LOX-IN-2 是一种 12R-脂氧合酶 (12R-LOX) 的抑制剂。12R-LOX-IN-2 抑制咪喹莫特 (IMQ) 诱导银屑病角质形成细胞过度增殖,并抑制细胞集落形成。12R-LOX-IN-2 还降低 IMQ 诱导细胞中 Ki67 的蛋白水平和 IL-17A 的 mRNA 表达。12R-LOX-IN-2 可用于牛皮癣和其他皮肤相关炎症性疾病的研究。
T24094 Glycerophosphoinositol lysine

Distinctive gpi lysine,Gpi lysine

Glycerophosphoinositol lysine has an anti-dandruff, anti-inflammatory, anti-aging activity. It significantly suppresses UVB - induced PGE secretion in NHEK keratinocytes.
T68470 ASB-16165

ASB-16165 is a phosphodiesterase 7A inhibitor that impairs proliferation of keratinocytes in vitro and in vivo. Inhibitors of PDE7A including ASB16165 might be useful for the treatment of psoriasis.
T31126 CX-659S

CX659S,UNII-YG2F04AVMQ,CX 659S

CX-659S is a novel diaminuracil derivative that indirectly inhibits Langerhans cell function by blocking the MEK1/2 -- ERK1/2 pathway in keratinocytes. CX-659S can inhibit the contact hypersensitivity induced by haptens in mice.
T80280 TLN-58

TLN-58是一种抗菌肽,对S. aureus、S. epidermidis和group A Streptococcus显示出抗菌活性。此外,TLN-58能够在正常人角质形成细胞及NCL-SG3细胞中诱导炎症细胞因子mRNA的上调。
T35452 β-Defensin-3 (human) (trifluoroacetate salt)

β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It inhibits the growth of the periodontopathogenic and cariogenic bacteria F. nucleatum, S. mutans, S. sobrinus, S. salivarius, and L. casei (MICs = 12.5-100 mg/l). It also inhibits the growth of S. aureus, S. pyogenes, P. aeruginosa, E. coli, and C. albicans. β-Defensin-3 stimulates gene expression and production of IL-6, IL-10, CXC...
T36004 1-O-Hexadecyl-sn-glycerol

1-O-Hexadecyl-sn-glycerol,(S)-(+)-Chimyl Alcohol,α-Chimyl Alcohol

1-O-Hexadecyl-sn-glycerol is a bioactive alkyl glyceryl ether. It reduces UVB-induced cell death and production of reactive oxygen species (ROS) and prostaglandin E2 in normal human epidermal keratinocytes (NHEKs). 1-O-Hexadecyl-sn-glycerol (50 μM) increases coronary flow and left ventricular developed pressure and reduces malondialdehyde (MDA) formation ex vivo in a rat heart model of ischemia/reperfusion injury. [2].Maulik, N., Tosaki, A., Engelman, R.M., et al. Myocardial salvage by chimyl al...
T35453 β-Defensin-4 (human) (trifluoroacetate salt)

β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and pro...
TP1540 Jagged-1 (188-204)

Jagged-1 188-204

Gamma-secretase Neuroscience; Proteases/Proteasome; Stem Cells
Jagged-1 (188-204) 是 JAG-1 蛋白的一个片段。其中 JAG-1 能够诱导单核细胞衍生的人树突状细胞成熟,是一种在培养的和原发性多发性骨髓瘤细胞中高度表达的 Notch 配体。
T35553 Ganglioside GQ1b Mixture (sodium salt)

Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes throu...
T83457 12R-LOX-IN-1

12R-LOX-IN-1(Compound 4a)是一种效能为IC50: 28.25 μM的12R-LOX抑制剂。该化合物能够有效抑制Imiquimod诱导的银屑病角质形成细胞的异常增殖和集落形成能力,同时减少活性氧、Ki67、IL-17A、TNF-α和IL-6的生成,适用于抗银屑病研究。
T36671 C2 Phytoceramide (t18:0/2:0)

C2 Phytoceramide is a bioactive semisynthetic sphingolipid that inhibits formyl peptide-induced oxidant release (IC50 = 0.38 μM) in suspended polymorphonuclear cells. It increases COX-2 protein levels 15-fold through ERK signaling. It induces death of keratinocytes (20% viability) with an ED50 value of 30 μM, the same concentration at which 35% of cells in a TUNEL assay are apoptotic. C2 Phytoceramide also has antiproliferative effects in CHO cells, with greater than 80% cytotoxicity achieved at...
T80090 Lugdunin

Antibiotic Microbiology/Virology
Lugdunin是一种具有抗菌活性的肽类抗生素。该化合物能够通过破坏细菌细胞膜的电位来抑制革兰氏阳性菌的生长,特别是对金黄色葡萄球菌(Staphylococcus aureus)表现出高效能,有效降低其在皮肤和鼻腔的定植能力。此外,Lugdunin还能在人类角质形成细胞和小鼠皮肤中促进LL-37和CXCL8/MIP-2的表达。
T69395 Nicotinamide-d4

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosyl...
T36379 Halometasone

Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8...
T35406 α-MSH TFA

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube fo...
T83744 Tiger17 TFA

H-Trp-Cys-Lys-Pro-Lys-Pro-Lys-Pro-Arg-Cys-His-NH2

Tiger17是一种环状肽,属于tigerinin-RC1和tigerinin-RC2的衍生物,这两种化合物是在螃蟹吃蛙(F. cancrivora)皮肤分泌物中发现的抗微生物肽。在5至20µg/ml的浓度范围内使用时,Tiger17能增加HaCaT角质形成细胞和人类皮肤成纤维细胞的增殖,并且在20µg/ml的浓度下增加HaCaT细胞的迁移。此外,Tiger17还能增加RAW 264.7巨噬细胞的招募及其TGF-β1和IL-6的分泌。在全层皮肤创伤的小鼠模型中,局部应用20µg/ml的Tiger17能加速伤口闭合和重新上皮化的速度。
T35451 β-Defensin-2 (human) (trifluoroacetate salt)

β-Defensin-2 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts.1It inhibits the growth of periodontopathogenic and cariogenic bacteria, includingP. gingivalisandS. salivarius.2β-Defensin-2 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes.3It also stimulates calcium mobilization, migration, and proliferation of keratinocytes whe...
T83735 Pap12-6 TFA

Pap12-6是一种从蝶类P. xuthus幼虫中发现的papiliocin十二个N-端氨基酸衍生的抗菌肽。它对包括E. coli、P. aeruginosa和S. syphimurium在内的八种革兰氏阴性细菌(MIC50s = 4-8 µM)以及革兰氏阳性细菌S. aureus、耐甲氧西林的S. aureus 3126(MRSA-3126)、B. subtilis和S. epidermidis(MIC50s = 4-8 µM)具有活性,但在25 µM浓度下不影响人类红细胞、小鼠RAW 264.7巨噬细胞、人类HaCaT角质形成细胞或人类HEK293肾细胞的活性。Pap12-6在4和8 µM浓度下可引起E. coli的膜去极化。Pap12-6(10 µM)预处理可降低LPS刺激的RAW 264.7巨噬细胞中一氧化氮(NO2-)、Tnf-α和Il-6的分泌水平。在体内,Pap12-6(10 mg/kg)可以提高感染E. coli的小鼠的存活率,并且在剂量为1 mg/kg时减少感染E. coli小鼠的肺、肝和肾中菌落形成单位(CFUs)的数量。Pap12-6(1 mg/kg)在E. co...

化合物

STIMA-1
Cat.No: T67858
Synonym: 2-Vinylquinazolin-4-ol,p53 Activator VII
Target: Others
GNF351
Cat.No: T15410
Synonym:
Target: Aryl Hydrocarbon Receptor
Efalizumab
Cat.No: T76924
Synonym: Hu1124,HU 1124
Target: Integrin
Jagged-1 (188-204) TFA(219127-21-6 free base)
Cat.No: TP1293
Synonym: Jagged-1 (188-204) TFA
Target: Gamma-secretase
12R-LOX-IN-2
Cat.No: T77677
Synonym:
Target: Lipoxygenase
Glycerophosphoinositol lysine
Cat.No: T24094
Synonym: Distinctive gpi lysine,Gpi lysine
Target:
ASB-16165
Cat.No: T68470
Synonym:
Target:
CX-659S
Cat.No: T31126
Synonym: CX659S,UNII-YG2F04AVMQ,CX 659S
Target:
TLN-58
Cat.No: T80280
Synonym:
Target:
β-Defensin-3 (human) (trifluoroacetate salt)
Cat.No: T35452
Synonym:
Target:
1-O-Hexadecyl-sn-glycerol
Cat.No: T36004
Synonym: 1-O-Hexadecyl-sn-glycerol,(S)-(+)-Chimyl Alcohol,α-Chimyl Alcohol
Target:
β-Defensin-4 (human) (trifluoroacetate salt)
Cat.No: T35453
Synonym:
Target:
Jagged-1 (188-204)
Cat.No: TP1540
Synonym: Jagged-1 188-204
Target: Gamma-secretase
Ganglioside GQ1b Mixture (sodium salt)
Cat.No: T35553
Synonym:
Target:
12R-LOX-IN-1
Cat.No: T83457
Synonym:
Target:
C2 Phytoceramide (t18:0/2:0)
Cat.No: T36671
Synonym:
Target:
Lugdunin
Cat.No: T80090
Synonym:
Target: Antibiotic
Nicotinamide-d4
Cat.No: T69395
Synonym:
Target:
Halometasone
Cat.No: T36379
Synonym:
Target:
α-MSH TFA
Cat.No: T35406
Synonym:
Target:
Tiger17 TFA
Cat.No: T83744
Synonym: H-Trp-Cys-Lys-Pro-Lys-Pro-Lys-Pro-Arg-Cys-His-NH2
Target:
β-Defensin-2 (human) (trifluoroacetate salt)
Cat.No: T35451
Synonym:
Target:
Pap12-6 TFA
Cat.No: T83735
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T6S0923 Hypericin

Hypericine,金丝桃素,Cyclosan

Apoptosis; Antiviral; Influenza Virus; Tyrosine Kinases; Antibacterial; PKC Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; Microbiology/Virology; Tyrosine Kinase/Adaptors
Hypericin (Cyclosan) 是贯叶连翘的提取物,有抗菌、抗病毒、抗肿瘤和抗抑郁作用。
TN2286 Tsugaric acid A

NO Synthase Immunology/Inflammation
Tsugaric acid A 能够显著抑制超氧阴离子的形成,还可以保护人类角质形成细胞,使其免受紫外线 B 诱导的损害。
TN1675 Gardenin B

栀子黄素B

Apoptosis; ROS; Caspase; NO Synthase Apoptosis; Immunology/Inflammation; Proteases/Proteasome
Gardenin B 是从Baccharis scandens 中分离出的一种黄酮类天然产物。它对肺、乳腺、结肠、肝和白血病细胞系以及角质形成细胞具有优异的抗增殖活性。
T3717 Hinokitiol

4-Isopropyltropolone,桧木醇,β-thujaplicin,β-桧木醇

DNA Methyltransferase; Virus Protease; Estrogen/progestogen Receptor; Nrf2 Chromatin/Epigenetic; Endocrinology/Hormones; Immunology/Inflammation; Microbiology/Virology
Hinokitiol (4-Isopropyltropolone) 是从日本扁柏中分离到的一种挥发油成分,可抑制紫外线 B 诱导的角质形成细胞凋亡,可调节雌激素受体信号传导并抑制人乳腺癌细胞的增殖。它具有抗感染、抗氧化及抗肿瘤等活性。
T5S1286 (+)-Columbianetin

二氢山芹醇,(S)-Columbianetin,Columbianetin

Antifungal Microbiology/Virology
(+)-Columbianetin ((S)-Columbianetin) 是 Columbianetin 的异构体。其中Columbianetin 是一种植物抗毒素,与芹菜贮藏过程中对病原体的抗性有关,具有良好的抗真菌和抗炎作用。
T6S1572 Sauchinone

ERK; p38 MAPK; NF-κB MAPK; NF-κB
Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS,TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。
T24025 Eckol

Eckol inhibits ultraviolet B-induced cell damage by a decrease in oxidative stress in human keratinocytes.
TN1235 3,4,5-Tricaffeoylquinic acid

TNF; Akt; HIV Protease Apoptosis; Cytoskeletal Signaling; Microbiology/Virology; PI3K/Akt/mTOR signaling; Proteases/Proteasome
3,4,5-Tricaffeoylquinic acid may attenuate the TNF-α±- and LPS-stimulated production of inflammatory mediators in keratinocytes by suppressing the Toll-like receptor 4 expression-mediated activation of the Akt, ERK and NF-κB pathways, it may exert an inhibitory effect against the pro-inflammatory mediator-induced skin disease.
T13670L (Z)-Ligustilide

藁本内酯,cis-Ligustilide,Ligustilide A,蒿本内酯 A

Antibacterial Microbiology/Virology
(Z)-Ligustilide (Ligustilide A) 是从川芎中提取的天然产物,具有抗菌和抗真菌活性。它抑制 FATP5 和 DGAT 的表达,抑制小鼠脂肪酸的摄取和酯化,有潜力研究非酒精性脂肪性肝病。
T38036 Lumisterol

Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities[1]. [1]. Anyamanee Chaiprasongsuk, et al. Protective Effects of Novel Derivatives of Vitamin D 3 and Lumisterol Against UVB-induced Damage in Human Keratinocytes Involve Activation of Nrf2 and p53 Defense Mechanisms. Redox Biol. 2019 Jun;24:101206.

天然产物

Hypericin
Cat.No: T6S0923
Synonym: Hypericine,金丝桃素,Cyclosan
Target: Apoptosis, Antiviral, Influenza Virus, Tyrosine Kinases, Antibacterial, PKC
Tsugaric acid A
Cat.No: TN2286
Synonym:
Target: NO Synthase
Gardenin B
Cat.No: TN1675
Synonym: 栀子黄素B
Target: Apoptosis, ROS, Caspase, NO Synthase
Hinokitiol
Cat.No: T3717
Synonym: 4-Isopropyltropolone,桧木醇,β-thujaplicin,β-桧木醇
Target: DNA Methyltransferase, Virus Protease, Estrogen/progestogen Receptor, Nrf2
(+)-Columbianetin
Cat.No: T5S1286
Synonym: 二氢山芹醇,(S)-Columbianetin,Columbianetin
Target: Antifungal
Sauchinone
Cat.No: T6S1572
Synonym:
Target: ERK, p38 MAPK, NF-κB
Eckol
Cat.No: T24025
Synonym:
Target:
3,4,5-Tricaffeoylquinic acid
Cat.No: TN1235
Synonym:
Target: TNF, Akt, HIV Protease
(Z)-Ligustilide
Cat.No: T13670L
Synonym: 藁本内酯,cis-Ligustilide,Ligustilide A,蒿本内酯 A
Target: Antibacterial
Lumisterol
Cat.No: T38036
Synonym:
Target:
TargetMol Loading
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