40
16
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T9927 |
Panitumumab
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Panitumumab 是一种重组全人源 IgG2 单克隆抗体,可与表皮生长因子(EGFR)结合,具有抗肿瘤活性。 | |||
T2670 |
ML167
NCGC00188654,CID44968231 |
DYRK; CDK | Cell Cycle/Checkpoint; Tyrosine Kinase/Adaptors |
ML167 (CID44968231) 是一种高选择性的 Cdc2 样激酶 4 抑制剂,IC50为 136 nM。 | |||
T1502 |
Vildagliptin
维达列汀,NVP-LAF 237,维格列汀,LAF237 |
Apoptosis; Ferroptosis; Proteasome; DPP-4 | Apoptosis; Proteases/Proteasome; Ubiquitination |
Vildagliptin (LAF237) 是一种选择性二肽基肽酶IV (DPP-IV) 抑制剂,在人 Caco-2 细胞中抑制 DPP-IV 的IC50为 3.5 nM。它具有出色的口服生物利用度和降血糖活性。 | |||
T0242L |
Sitagliptin phosphate monohydrate
MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物 |
Proteasome; DPP-4; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP-IV 抑制剂,在 Caco-2 细胞提取物中的 IC50 为 19 nM。 | |||
T34973 |
Tyrphostin 8
4-Hydroxybenzylidenemalononitrile |
EGFR; GTPase | Angiogenesis; GPCR/G Protein; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Tyrphostin 8(4-Hydroxybenzylidenemalononitrile) 是一种有效的 GTP 酶抑制剂,对 EGFR 激酶有抑制作用, IC50 值为 560 μM。Tyrphostin 8 可抑制蛋白丝氨酸/苏氨酸钙调磷酸酶 (IC50=21 μM),增强 Caco-2 细胞中转铁蛋白受体介导的转吞作用,并增加口服胰岛素 - 转铁蛋白的降血糖作用。 | |||
T3148 |
MK-571 sodium
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid |
Leukotriene Receptor; LTR | GPCR/G Protein; Immunology/Inflammation |
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂,在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。 | |||
T18957 |
D-Ala-Lys-AMCA hydrochloride
|
Others | Others |
D-Ala-Lys-AMCA hydrochloride 是发射蓝色荧光的质子偶联寡肽转运蛋白 1 (PEPT1) 的已知底物。 D-Ala-Lys-AMCA 可能被转运到 Caco-2 细胞和肝癌细胞中。 | |||
T23358 |
Sitagliptin phosphate
磷酸西他列汀,Januvia,MK-0431 phosphate,Sitagliptin (phosphate) |
DPP-4; Autophagy | Autophagy; Proteases/Proteasome |
Sitagliptin phosphate (MK-0431 phosphate) 是一种二肽基肽酶 4 (DPP4) 抑制剂,在 Caco-2 细胞中,IC50值为 19 nM。 | |||
T0242 |
Sitagliptin
西他列汀,MK0431,西格列汀 |
Proteasome; DPP-4; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Sitagliptin (MK0431) 是一种有效的 DPP4抑制剂,在 Caco-2 细胞中,IC50值为 19 nM。它是一种新型口服降糖药,可单独使用或与二甲双胍或噻唑烷二酮联合用于治疗 2 型糖尿病。 | |||
T37281 |
1-Palmitoleoyl glycerol
|
||
1-Palmitoleoyl glycerol 是具有生物活性的单酰基甘油,在 Caco-2 细胞中可抑制 P-糖蛋白,还能诱导胸腺细胞凋亡。 | |||
T81910 |
L-Tryptophanylglycine
|
||
L-Tryptophanylglycine(Trp-gly)作为一种二肽,其对Caco-2细胞摄取Ceronapril具有抑制作用,表现出Ki值为7.19 mM。 | |||
T40930 |
(S)-Sitagliptin phosphate
(S)-Sitagliptin phosphate,(S)-MK-0431 phosphate |
||
(S)-Sitagliptin phosphate, the less active S-enantiomer of Sitagliptin phosphate, is a high-potency inhibitor of DPP4. It exhibits an IC50 of 19 nM in Caco-2 cell extracts. | |||
T83083 |
Anticancer agent 166
|
||
Anticanceragent 166 (compound 3)表现出对Caco-2细胞的显著抑制效果,其半数抑制浓度(IC50)为9.6 nM。 | |||
T61076 |
Vildagliptin dihydrate
|
||
Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1]. | |||
T30491 |
BMS 183920
BMS-183920,BMS183920 |
||
BMS-183920 is a diacid, potent angiotensin II receptor antagonist that improves Caco-2 cell permeability and in vivo oral absorption. The relative degree of hydrolysis (biological activation) and prodrug metabolism determines whether substantial improveme | |||
T69897 |
MC-70 hydrochloride
|
||
MC-70 hydrochloride is a potent P-gp inhibitor with good selectivity towards BCRP pump (EC50 values 0.05 μM, 0.69 μM, 9.3 μM, and 73 μM for Caco-2, MDR1, MRP1, and BCRP inhibition, respectively). | |||
T32242 |
IWP-051
IWP051 |
||
IWP-051 is a potent, orally active sGC stimulator (EC50 = 290nM). IWP-051 showed >99% plasma protein binding, high metabolic stability, high permeability, and no efflux in a Caco-2 model of intestinal absorption. IWP-051 achieves good alignment of pote | |||
T61783 | Antimicrobial agent-1 | ||
Antimicrobial Agent-1 (compound 6C) shows strong activity (MIC = 2 μg/mL) against TolC mutant E. coli. Additionally, it synergistically interacts with Colistin to exhibit enhanced activity against Gram-negative bacteria. Importantly, Antimicrobial Agent-1 exhibits no cytotoxic effects on mammalian cell lines. Its MIC values on Caco-2 and Vero cell lines are greater than 128 μg/mL [1]. | |||
T82489 | eIF4E-IN-6 | ||
eIF4E-IN-6(化合物4b)是一种针对eIF4E设计的抑制剂,可阻止其与cap mRNA的结合,其化学结构为GMP类似物。该化合物在Caco-2、HepG-2和MCF-7细胞系中显示出细胞毒性效果,其IC50值分别约为31、27和21 μM。 | |||
T80142 |
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)
c(GRGDSP) |
Integrin | Cytoskeletal Signaling |
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro)(c(GRGDSP))为RGD 抑制肽。该化合物作为合成的α5β1整联蛋白配体,能够竞争性阻断 invasin(Inv)与Caco-2细胞表面α5β1整联蛋白的相互结合。 | |||
T82314 | GK444 | HDAC | Chromatin/Epigenetic; DNA Damage/DNA Repair |
GK444(Compound 15a),一种针对HDAC1/2的抑制剂,IC50分别为HDAC1和HDAC2的100 nM与92 nM。其对Caco-2细胞的IC50为4.1μM,并能下调原代正常人肺成纤维细胞中TGF-β1刺激的COL1A1 mRNA水平。此外,GK444还能抑制博来霉素诱发的小鼠肺纤维化。 | |||
T79256 |
DPP-4-IN-8
|
||
DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂,具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性,并剂量依赖性地降低 TNF-α、IL-6 和 IL-1β 的表达水平[1]。 | |||
T18959 |
D-Ala-Lys-AMCA
|
Others | Others |
D-Ala-Lys-AMCA is a known substrate of proton-coupled oligopeptide transporter 1 (PEPT1) that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into Caco-2 cells and liver cancer cells. | |||
T82617 |
D-Ala-Lys-AMCA TFA
|
||
D-Ala-Lys-AMCA是一个已知的PEPT1底物,具有发射蓝色荧光的性质。该化合物可被转运至肝癌细胞及Caco-2细胞。D-Ala-Lys-AMCA能够作为工具用于评估PEPT1的特异性底物或其抑制剂。 | |||
T35815 |
Vildagliptin carboxylic acid metabolite (trifluoroacetate salt)
|
||
Vildagliptin carboxylic acid metabolite is the major metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor vildagliptin in humans. Vildagliptin carboxylic acid metabolite has an IC50 value of 477 μM for DPP-4 in human Caco-2 cells. It is formed from hydrolysis of the cyano group on vildagliptin. | |||
T70908 |
EST64454 free base
|
||
EST64454 is a σ1 receptor (σ1R) antagonist clinical candidate for the treatment of pain. EST64454 shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability. | |||
T79915 |
Antioxidant agent-15
|
COX | Immunology/Inflammation; Neuroscience |
Antioxidant agent-15 (Compound 4) 显示出显著的抗氧化抑制活性,其 IC50 为 15.44 nM。在细胞水平上,Antioxidant agent-15 对Hela、Hep G2 和 Caco-2肿瘤细胞生长的抑制作用各自具有不同的 IC50 值,分别为 395.26 nM、4000.4 nM 和 24.6 nM。 | |||
T61504 | PKM2 activator 3 | ||
PKM2 activator 3 is a highly potent compound that activates PKM2, with an AC 50 value of 90 nM. It exhibits excellent Caco-2 permeability, a low efflux ratio, and remarkable microsomal stability. PKM2 activator 3 is particularly valuable for anticancer research purposes [1]. (AC 50: the concentration at which 50% enzyme activation occurs.) | |||
T78793 |
MAOA-IN-1
|
Monoamine Oxidase | Neuroscience |
MAOA-IN-1(化合物15)是一种口服有效的MAOA抑制剂,对前列腺癌细胞显示出细胞毒性。该化合物表现出Caco-2渗透性,同时具有较低的CNS渗透性。MAOA-IN-1可以用于研究抗癌和抗炎适应症。 | |||
T18958 |
D-Ala-Lys-AMCA TFA (375822-19-8 free base)
D-Ala-Lys-AMCA TFA |
Others | Others |
D-Ala-Lys-AMCA hydrochloride is a known substrate of proton-coupled oligopeptide transporter 1 (PEPT1) that emits blue fluorescence. D-Ala-Lys-AMCA may be transported into Caco-2 cells and liver cancer cells. | |||
T36410 |
9(E),11(E),13(E)-Octadecatrienoic Acid
|
||
9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces a... | |||
T38072 | HSGN-218 | ||
HSGN-218 is a gut-restrictive antibiotic.1It is active againstC. difficile(MIC = 0.007 μg/ml) and clinical isolates ofC. difficile(MICs = 0.003-0.03 μg/ml) and is not cytotoxic to Caco-2 cells when used at concentrations ranging from 4 to 64 μg/ml. HSGN-218 (50 mg/kg) increases survival and protects mice fromC. difficilerecurrence in mouse models ofC. difficileinfection. 1.Naclerio, G.A., Abutaleb, N.S., Li, D., et al.Ultrapotent inhibitor of Clostridioides difficile growth, which suppresses rec... | |||
T36035 |
CAY10784
|
||
CAY10784 is a STAT3 inhibitor (IC50= 0.74 μM in a reporter assay) and a derivative of WP1066 .1It inhibits proliferation of HeLa, Caco-2, A549, A375, U87MG, and HL-60 cancer cells (IC50s = 1.8, 1.8, 3, 2.8, 2.3, and 1.2 μM, respectively) but not PC3 or HT-29 cancer cells (IC50s = >10 μM for both). CAY10784 is also active againstH. pyloriandC. jejuni(MICs = 1.6 and 4.7 μM, respectively).2 1.Lü, Z., Li, X., Li, K., et al.Structure-activity study of nitazoxanide derivatives as novel STAT3 pathway i... | |||
T36698 |
9(Z),11(E),13(E)-Octadecatrienoic Acid
|
||
9(Z),11(E),13(E)-Octadecatrienoic Acid (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1... | |||
T36887 |
8(E),10(E),12(Z)-Octadecatrienoic Acid
|
||
8(E),10(E),12(Z)-Octadecatrienoic acid is a conjugated polyunsaturated fatty acid (PUFA) that has been found inC. officinalisseed oil and has anticancer activity.1,2,3It inhibits the growth of Caco-2 cells when used at concentrations ranging from 10 to 50 μM.28(E),10(E),12(Z)-Octadecatrienoic acid (10 μM) induces formation of thiobarbituric acid reactive substances (TBARS) and apoptosis in DLD-1 colorectal adenocarcinoma cells.3It also inhibits prostaglandin biosynthesis in sheep vesicular gland... | |||
T36517 |
Resveratrol-3-O-sulfate sodium
|
||
Resveratrol-3-O-sulfate is a metabolite of resveratrol . In U-937 cells stimulated with LPS, resveratrol-3-O-sulfate (1 μM) decreases the expression of IL-1α, IL-1β, and IL-6 by 61.2, 76.6, and 42.2%, respectively, and decreases the release of TNF-α and IL-6 to similar levels as resveratrol. It has antioxidant activity in a Trolox assay, dose-dependently decreases growth of Caco-2 colorectal adenocarcinoma cells when used at concentrations ranging from 10 to 100 μM, and induces apoptosis at conc... | |||
T35775 |
HT-2 Toxin-13C22
HT-2 Toxin-13C22 |
||
HT-2 toxin-13C22is intended for use as an internal standard for the quantification of HT-2 toxin by GC- or LC-MS. HT-2 toxin is a type A trichothecene mycotoxin and an active, deacetylated metabolite of the trichothecene mycotoxin T-2 toxin .1,2Like T-2 toxin, HT-2 toxin inhibits protein synthesis and cell proliferation in plants.2HT-2 toxin also reduces viability of HepG2, A549, HEp-2, Caco-2, A-204, U937, Jurkat, and RPMI-8226 cancer cells with IC50values ranging from 3.1 to 23 ng/ml and human... | |||
T36889 |
Methyl alpha-eleostearate
|
||
Methyl alpha-eleostearate (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPARγ. In DLD-1 cells supple... | |||
T36888 |
9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester
|
||
9(Z),11(E),13(E)-Octadecatrienoic Acid ethyl ester (α-ESA) is a conjugated polyunsaturated fatty acid commonly found in plant seed oil. This fatty acid accounts for about 60% of the total fatty acid composition of bitter gourd seed oil and about 70% in tung oil. α-ESA is metabolized and converted to conjugated linoleic acid (9Z,11E-CLA) in rats. It has shown potential as a tumor growth suppressor. In colon cancer Caco-2 cells, α-ESA induced apoptosis through up-regulation of GADD45, p53, and PPA... | |||
T61259 |
Valganciclovir
|
||
Valganciclovir 是ganciclovir 的原药,具有抗巨细胞病毒CMV 感染的活性。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TQ0265 |
Indolelactic acid
|
Endogenous Metabolite | Metabolism |
Indolelactic acid 是 Azotobacter vinelandii 培养中的色氨酸分解代谢物。 | |||
T19676 |
Tributyrin
NSC661583,NSC 661583,NSC-661583,甘油三丁酸酯 |
Apoptosis | Apoptosis |
Tributyrin (Glyceryl tributyrate) 是一种中性短链脂肪酸甘油三酯,是一种稳定且吸收迅速的丁酸前药。 它通过生物膜扩散并被细胞内脂肪酶代谢,在体内将有效的丁酸直接释放到细胞中,有抗增殖、促凋亡和诱导分化作用。 | |||
T7210 |
Guanosine 5'-diphosphate
GDP,鸟苷-5ˊ-二磷酸 |
Endogenous Metabolite | Metabolism |
Guanosine 5'-diphosphate (GDP) 是核苷二磷酸,是潜在的铁动员剂,能够阻断铁调素-铁转运蛋白相互作用并调节白细胞介素-6 (IL-6)/stat-3 途径。 | |||
TN1237 |
3-O-Methylgallic acid
3,4-Dihydroxy-5-methoxybenzoic acid,3-O-甲基没食子酸 |
Apoptosis; NF-κB; OCT; DNA/RNA Synthesis; STAT | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Membrane transporter/Ion channel; NF-κB; Stem Cells |
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) 是一种花青素代谢产物,具有强大的抗氧化能力。它还诱导细胞凋亡并具有抗癌作用,可抑制 Caco-2 细胞增殖,IC50值为 24.1 μM。 | |||
TN3967 | Epieriocalyxin A | ERK; BCL; ROS; Caspase; DNA/RNA Synthesis; JNK | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Immunology/Inflammation; MAPK; Proteases/Proteasome |
Epieriocalyxin A 可以抑制 Caco-2 结肠癌细胞的生长。它可能是未来结肠癌治疗的潜在药物。 | |||
TN1740 |
Homoeriodictyol
高胜草酚,高圣草酚 |
5-HT Receptor; transporter; Sodium Channel; Drug Metabolite | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience |
Homoeriodictyol 是 Eriocitrin 的代谢物,属于黄酮类。Eriocitrin 是强效抗氧化剂。 | |||
T5S0890 |
Oleandrin
Neriostene,Folinerin,Foliandrin,欧夹竹桃苷 |
Apoptosis; ATPase; Potassium Channel; Sodium Channel | Apoptosis; Membrane transporter/Ion channel |
Oleandrin (Folinerin) 是夹竹桃属中的一种类固醇,可抑制Na+/K+-ATPase 活性,IC50为 620 nM。 | |||
T36473 |
trans-Nerolidol
|
||
trans-Nerolidol is a sesquiterpene that has been found in various plants, includingC. sativa, and has diverse biological activities, including antimicrobial, antioxidant, anticancer, and insecticidal properties.1,2,3,4In a disc assay,trans-nerolidol inhibits the growth ofS. aureus,B. subtilis,E. coli, andS. cerevisiaewith zones of inhibition measuring 10, 9, 10, and 4 mm, respectively.2It reduces viability of CaCo-2 adenocarcinoma cells with an IC50value of 28.7 mg/L and reduces production of re... | |||
T6S1315 |
Oroxylin A
千层纸素A,6-Methoxybaicalein,Baicalein 6-methyl ether |
Virus Protease; HIF/HIF Prolyl-Hydroxylase; Autophagy | Autophagy; Chromatin/Epigenetic; Metabolism; Microbiology/Virology |
Oroxylin A (Baicalein 6-methyl ether) 是一种有活性的黄酮,具有较强的抗癌作用。 | |||
T81797 |
Microcystin-LF
|
||
Microcystin-LF 是 Microcystin-LR 的苯丙氨酸变体,属于细菌代谢物,且对 Caco-2 细胞显示出细胞毒性。 | |||
TN1387 |
Angelol B
|
Others | Others |
The absorption and transport of angelol A and Angelol B are passive diffusion as the dominating process in Caco-2 cell monolayer model. | |||
TN1386 |
Angelol A
当归酚A,当归醇A |
Others | Others |
Angelol A and angelol B are passive diffusion as the dominating process in Caco-2 cell monolayer model. | |||
TQ0164 |
Dodecanoic acid ingenol ester
正十二烷酸巨大戟酯,13-Oxyingenol dodecanoat |
Others | Others |
Dodecanoic acid ingenol ester, a natural compound, shows moderate cytotoxicity with IC50 values being 35.59 μM (Caco-2), 24.04 μM (MCF-7), and 22.24 μM (MCF-7/ADM). | |||
TN6645 | Lucidumol A | ||
Lucidumol A has relatively good effect against aldose reductase with IC50 of 19.1uM. Lucidumol A has cytotoxic activity, it reduced cell growth in three human carcinoma cells (Caco-2, HepG2, and HeLa cells) dose dependently with LC50s from 20.87 to 84.36 | |||
T37810 |
6',7'-Epoxybergamottin
|
||
6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo... | |||
TN2190 |
Scoulerine
|
Apoptosis; Beta-Secretase; BACE; Parasite | Apoptosis; Microbiology/Virology; Neuroscience |
Scoulerine 是抗有丝分裂化合物。它抑制细胞增殖,阻止细胞周期,并诱导癌细胞凋亡。它也是BACE1(淀粉样前体蛋白裂解酶 1) 的抑制剂。 |