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11

抑制剂 & 化合物

4

天然产物

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Cat. No. Product Name Target Signaling Pathways
T7263 SMS2-IN-2

SMS2 inhibitors

Others Others
SMS2-IN-2 (SMS2 inhibitors) 是一种具有高度选择性、口服具有活力的鞘磷脂合成酶 2 抑制剂,能够作用于 SMS2 (IC50:100 nM)和 SMS1 (IC50:56 nM)。它可减轻慢性炎症反应。
T21314 Amsilarotene

TAC-101,TAC 101,TAC101

CDK Cell Cycle/Checkpoint
Amsilarotene (TAC101) 是口服有活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡,可用于研究癌症。
T35610 2,5-dimethyl Celecoxib

Apoptosis; Wnt/beta-catenin; Prostaglandin Receptor Apoptosis; Cytoskeletal Signaling; GPCR/G Protein; Immunology/Inflammation; Stem Cells
2,5-dimethyl Celecoxib 是塞来昔布衍生物和微粒体前列腺素 E 合酶 1 (mPGES-1) 的靶向抑制剂,mPGES-1 是炎症介质 PGE2 合成途径中的关键酶。
T37903 Deoxynojirimycin Tetrabenzyl Ether

Deoxynojirimycin (dNM) tetrabenzyl ether is an intermediate for the synthesis of glucosylceramide synthase inhibitors such as 1-dNM, a glucose analog that potently inhibits α-glucosidase I and II.
T63401 EGFR/HER2/TS-IN-1

EGFR/HER2/TS-IN-1 是 EGFR、HER2和TS (Thymidylate synthase)抑制剂,他们的IC50值分别为 0.203、0.088 和 0.168 μM,具有诱导 MCF7 细胞凋亡(apoptosis)的作用。
T36015 PDMP (hydrochloride)

PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
TP2195 Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell

Others Others
Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell (Ac-Pro-Tyr-Asn-Ser-Ser-Pro-Arg-Pro-Glu-Gln-His-Lys-Ser-Tyr-Lys-Cys) is a peptide that inhibits the function of NOSs as a result it blocks the production of NO. Because of the invol
T35979 Benastatin C

Benastatin C is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2It inhibits glutathione S-transferase (GST; IC50= 24 μg/ml for the rat liver enzyme).2Benastatin C also inhibits the esterase activity of isolated porcine pancreatic lipase (IC50= 10 μg/ml). It increases LPS- or concanavalin A-induced blastogenesis of isolated mouse spleen lymphocytes in a concentration-dependent manner. 1.Xu, Z., Schenk, A., and Hertweck, C.Molecul...
T36974 D-threo-PPMP hydrochloride

D-threo-PPMP is a glucosylceramide (GlyCer) synthetase inhibitor.1,2It is the active enanantiomer and enzymatic inhibitory component of the racemic DL-threo-PPMP . In MDCK kidney epithelial cells, D-threo-PPMP induces a 70% reduction in cell growthin vitroat 20 μM and significantly inhibits DNA synthesis at 3 μM.3[Matreya, LLC. Catalog No. 1865] 1.Shen, W., Henry, A.G., Paumier, K.L., et al.Inhibition of glucosylceramide synthase stimulates autophagy flux in neuronsJ. Neurochem.129(5)884-894(201...
T35978 Benastatin A

Benastatin A is a polyketide synthase-derived benastatin that has been found inStreptomycesand has diverse biological activities.1,2,3It inhibits glutathione S-transferase (GST; Ki= 5 μM for the rat liver enzyme).2Benastatin A is active against several bacteria, including methicillin-resistantS. aureus(MRSA; MIC = 3.12 μg/ml). It induces apoptosis and cell cycle arrest at the G1/G0phase in Colon 26 mouse colon cancer cells when used at concentrations of 20 and 16 μM, respectively.3 1.Xu, Z., Sch...
T35560 SAR502250

SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD)[1][2]. SAR502250 (0.01-1 μM; 36 h) attenuates the Aβ25-35-induced cell death in rat embryonic hippocampal neurons[2]. SAR502250 (1-100 mg/kg; a single p.o,) attenuates tau hyperphosphorylation in the cortex and spinal cord of transgenic mic...

化合物

SMS2-IN-2
Cat.No: T7263
Synonym: SMS2 inhibitors
Target: Others
Amsilarotene
Cat.No: T21314
Synonym: TAC-101,TAC 101,TAC101
Target: CDK
2,5-dimethyl Celecoxib
Cat.No: T35610
Synonym:
Target: Apoptosis, Wnt/beta-catenin, Prostaglandin Receptor
Deoxynojirimycin Tetrabenzyl Ether
Cat.No: T37903
Synonym:
Target:
EGFR/HER2/TS-IN-1
Cat.No: T63401
Synonym:
Target:
PDMP (hydrochloride)
Cat.No: T36015
Synonym:
Target:
Nitric Oxide Synthase (599-613) Blocking Peptide, Bovine Endothelial Cell
Cat.No: TP2195
Synonym:
Target: Others
Benastatin C
Cat.No: T35979
Synonym:
Target:
D-threo-PPMP hydrochloride
Cat.No: T36974
Synonym:
Target:
Benastatin A
Cat.No: T35978
Synonym:
Target:
SAR502250
Cat.No: T35560
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0983 Penicillamine

青霉胺,d-penicillamin,Dimethyl Cysteine,D-青霉胺,Artamine,D-(-)-Penicillamine

Antibiotic Microbiology/Virology
Penicillamine (Artamine) 是一种 penicillin 的代谢降解产物,是一种螯合剂,可作用于威尔逊氏病。
T4S0145 Corylifol A

Corylinin,补骨脂异黄酮A

hCE; STAT; UGT JAK/STAT signaling; Metabolism; Stem Cells
Corylifol A (Corylinin) 是补骨脂中的一种天然产物,可抑制IL-6 诱导的STAT3激活和磷酸化,IC50值为0.81 μM。
TJS0387 Desoxyrhaponticin

去氧土大黄苷,Deoxyrhapontin,脱氧土大黄苷,Deoxyrhaponticin

Apoptosis; Fatty Acid Synthase Apoptosis; Metabolism
Desoxyrhaponticin (Deoxyrhaponticin) 是来自西藏营养食品唐古特大黄中的一种二苯乙烯苷。它是脂肪酸合成酶抑制剂,抑制细胞内 FAS 活性,下调人乳腺癌 MCF-7细胞中 FAS 的表达。它是控制糖尿病餐后高血糖的潜在药物。
TN1365 Albaspidin AP

Fatty Acid Synthase Metabolism
Albaspidin-AP, -PP, -PB inhibit Fatty acid synthase (FAS) with IC50 values ranging from 23.1+/-1.4 to 71.7+/-3.9 microM, they could be considered to be a promising class of FAS inhibitors, and FAS is emerging as a potential therapeutic target to treat can

天然产物

Penicillamine
Cat.No: T0983
Synonym: 青霉胺,d-penicillamin,Dimethyl Cysteine,D-青霉胺,Artamine,D-(-)-Penicillamine
Target: Antibiotic
Corylifol A
Cat.No: T4S0145
Synonym: Corylinin,补骨脂异黄酮A
Target: hCE, STAT, UGT
Desoxyrhaponticin
Cat.No: TJS0387
Synonym: 去氧土大黄苷,Deoxyrhapontin,脱氧土大黄苷,Deoxyrhaponticin
Target: Apoptosis, Fatty Acid Synthase
Albaspidin AP
Cat.No: TN1365
Synonym:
Target: Fatty Acid Synthase
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