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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T19672	Amtolmetin guacil MED 15,MED15,ST679,呱氨托美丁,ST-679,ST 679,MED-15	COX	Immunology/Inflammation; Neuroscience
	Amtolmetin guacil (ST-679) 抑制前列腺素合成和环氧合酶。 Amtolmetin guacil 具有与托美汀类似的 NSAID 特性，具有额外的镇痛、解热和胃保护特性。
T36682	USP30 inhibitor 18	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	USP30 inhibitor 18 是有效的USP30选择性抑制剂，IC50为 0.02 μM。它增加蛋白质泛素化并加速线粒体自噬。
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T36436	Spergualin trihydrochloride
	Spergualin trihydrochloride is a natural product that first identified as an antibiotic from culture filtrates of Bacillus laterosporus BMG162-aF2[1]. Spergualin trihydrochloride derivatives likely acts as Hsp70 modulators[1]. [1]. Srikanth Patury, et al. Pharmacological Targeting of the Hsp70 Chaperone. Curr Top Med Chem. 2009;9(15):1337-51.
T38127	pNPS-DHA
	pNPS-DHA is an arylamide derivative of docosahexaenoyl ethanolamide that has anti-allergic activity.1It inhibits degranulation of RBL-2H3 mast cells (IC50= 15 μM).pNPS-DHA (1,000 mg/kg) inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) in mice. 1.Kim, I.-H., Kanayama, Y., Nishiwaki, H., et al.Structure-activity relationships of fish oil derivatives with anti-allergic activity in vitro and in vivoJ. Med. Chem.62(21)9576-9592(2019)
T38292	4-(N-Boc-amino)piperidine
	4-(N-Boc-amino)piperidine is an organic building block.1,2It has been used in the synthesis of aminopiperidine antiviral chemokine (C-C motif) receptor 5 (CCR5) antagonists and antibacterial agents. 1.Burrows, J.N., Cumming, J.G., Fillery, S.M., et al.Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureasBioorg. Med. Chem. Lett.15(1)25-28(2005) 2.Reck, F., Alm, R., Brassil, P., et al.Novel N-linked aminopiperidine inhibitor...
T36782	TAK1-IN-2 TAK1-IN-2
	TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM[1]. TAK1-IN-2 (compound 54) (10 μM) has no effect on cell viability in TNF-α stimulated HCT-15 cells[1]. [1]. Veerman JJN, et, al. Discovery of 2,4-1 H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors. ACS Med Chem Lett. 2021 Mar 3;12(4):555-562.
T35679	2,4-Dichlorobenzenesulfonyl chloride
	2,4-Dichlorobenzenesulfonyl chloride is a heterocyclic building block.1It has been used in the synthesis of nicotinyl arylsulfonylhydrazides that have anticancer and antibacterial activitiesin vitro. 1.Kamal, A., Khan, M.N.A., Reddy, K.S., et al.Synthesis of a new class of 2-anilino substituted nicotinyl arylsulfonylhydrazides as potential anticancer and antibacterial agentsBioorg. Med. Chem.15(2)1004-1013(2007)
T36462	CAY10770 CAY10770
	CAY10770 is an inhibitor of the cytochrome P450 (CYP) isoform CYP4Z1 (IC50= 5.9 μM).1It is selective for CYP4Z1 over CYP4A11, CYP4F2, CYP4F3a, CYP4F3b (IC50s = 187-282 μM) but does inhibit CYP4F8 and CYP4F12 (IC50s = 167 and 91 μM, respectively). CAY10770 (3 μM) inhibits the production of 14(15)-EET, 19-HETE, and 14(15)-DiHET by 83, 86, and 80%, respectively, in T47D breast cancer cells expressing CYP4Z1. 1.Kowalski, J.P., McDonald, M.G., Pelletier, R.D., et al.Design and characterization of the...
T36075	Cholic Acid anilide
	Cholic acid anilide is a synthetic bile acid and derivative of cholic acid that inhibits the germination of C. difficile strain R20291 spores in vitro (IC50 = 1.8 μM).1 \|1. Sharma, S.K., Yip, C., Esposito, E.X., et al. The design, synthesis, and characterizations of spore germination inhibitors effective against an epidemic strain of Clostridium difficile. J. Med. Chem. 61(15), 6759-6778 (2018).
T36658	Boc-Glu-OBzl
	Boc-Glu-OBzl is an amino acid building block.1,2It has been used in the synthesis of peptide-based inhibitors of human caspases and human rhinovirus (HRV) 3C protease that have enzyme inhibitory activityin vitro. 1.Garcia-Calvo, M., Peterson, E.P., Leiting, B., et al.Inhibition of human caspases by peptide-based and macromolecular inhibitorsJ. Biol. Chem.273(49)32608-32613(1998) 2.Dragovich, P.S., Webber, S.E., Babine, R.E., et al.Structure-based design, synthesis, and biological evaluation of i...
T35629	ATRA-BA Hybrid
	ATRA-BA hybrid is a mutual prodrug form of all-transretinoic acid and butyric acid .1ATRA-BA hybrid is cleaved to release ATRA and BA in isolated mouse plasma. It inhibits the growth of MDA-MB-231 breast and PC3 prostate cancer cells with GI50values of 0.01 and 1.02 μM, respectively. ATRA-BA (20 μM) has 15-fold greater antiproliferative activity in PC3 cells compared to an equimolar concentration of ATRA and BA. 1.Gediya, L.K., Khandelwal, A., Patel, J., et al.Design, synthesis, and evaluation o...
T36034	CAY10774
	CAY10774 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 (IC50= 15 nM in a homologous time-resolved fret (HTRF) assay).1It increases the activation of Jurkat cells expressing PD-1 in co-culture with artificial antigen-presenting cells (aAPCs) expressing PD-L1 (EC50= 6.6 μM in a reporter assay). CAY10774 increases surface expression of PD-1 on primary human CD4+and CD8+T cells co-cultured with aAPCs. 1.Konieczny, M., Musielak, B., Koc...
T37754	Avilamycin A
	Avilamycin A is an antibiotic.1 It is active against veterinary isolates of C. perfringens (MICs = ≤0.06-0.5 mg/L) and B. hyodysenteriae (MICs = 12.5-100 μg/ml).1,2 Dietary administration of avilamycin A (15 and 30 ppm) reduces mortality in a broiler cockerel model of C. perfringens infection.3 Formulations containing avilamycin A have been used in the prevention of necrotic enteritis in livestock. \|1. Watkins, K.L., Shryock, T.R., Dearth, R.N., et al. In-vitro antimicrobial susceptibility of Cl...
T35686	3-Acetyl Betulinaldehyde
	3-Acetyl betulinaldehyde is a triterpene and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inA. japonica.1It is an intermediate in the synthesis of 3-acetylbetulinic acid, as well as various lupine and germanicane triterpenes and saponins with anticancer activity.2 1.Tung, N.H., Kwon, H.-J., Kim, J.-H., et al.An anti-influenza component of the bark of Alnus japonicaArch. Pharm. Res.33(3)363-367(2010) 2.Thibeault, D., Gauthier, C., Legault, J., et al.Synthesis a...
T37414	CAY10771
	CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Ch...
T36096	Thiocoraline
	Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA sy...
T36215	17R(18S)-EpETE
	17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid .1,217R(18S)-EpETE is an activator of large-conductance calcium-activated potassium (BKCa) channels, increasing the potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells (VSMCs) at +60 mV when used at a concentration of 50 nM.2It has negative chronotropic effects in isolated neonatal rat cardiomyocytes (NRCMs; EC50= ~1-2 nM) and prevents calcium-induced increases ...
T36047	LH1307
	LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays). \|1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors o...
T36046	LH1306
	LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays). \|1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibito...
T35527	PI3Kα-IN-4 PI3Kα-IN-4
	PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit t...
T36418	O-Desmethyl-N-deschlorobenzoyl Indomethacin
	O-Desmethyl-N-deschlorobenzoyl indomethacin is a metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor indomethacin .1It is formed from indomethacin in isolated rabbit hepatocytes. O-Desmethyl-N-deschlorobenzoyl indomethacin (600 μM) decreases the viability of HL-60 leukemia cells when cultured with glucose oxidase.2It has also been used in the synthesis of prostaglandin D2receptor antagonists.3 1.Evans, M.A., Papazafiratou, C., Bhat, R., et al.Indomethacin metabolism ...
T38381	CAY17c
	CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620,...
T36722	Deltorphin II (trifluoroacetate salt)
	Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...
T36486	Benpyrine
	Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research[1]. Benpyrine (5-20 μM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abo...
T36629	Givinostat
	Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1...
T36012	p38α inhibitor 2
	p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. [1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of pr...
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...
T35591	Guanfacine-13C,15N3 Guanfacine-13C,15N3
	Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacin...
T35568	BODIPY-aminoacetaldehyde diethyl acetal
	BODIPY-aminoacetaldehyde diethyl acetal (BAAA-DA) is a stable precursor to BODIPY-aminoacetaldehyde, a cell-permeable fluorescent substrate for aldehyde dehydrogenase (ALDH).1,2BODIPY-aminoacetaldehyde diethyl acetal is converted under acidic conditions to BODIPY-aminoacetaldehyde (BAAA).2BAAA is cell-permeant and is converted intracellularly by ALDH to BODIPY aminoacetate (BAA), which is retained by cells and can be used to identify cells with high ALDH activity.1BAA is a substrate for the effl...

化合物

Amtolmetin guacil

Cat.No: T19672

Synonym: MED 15,MED15,ST679,呱氨托美丁,ST-679,ST 679,MED-15

Target: COX

USP30 inhibitor 18

Cat.No: T36682

Target: DUB

Cat.No: T36968

Target: Topoisomerase

Spergualin trihydrochloride

Cat.No: T36436

Cat.No: T38127

4-(N-Boc-amino)piperidine

Cat.No: T38292

Cat.No: T36782

Synonym: TAK1-IN-2

2,4-Dichlorobenzenesulfonyl chloride

Cat.No: T35679

Cat.No: T36462

Synonym: CAY10770

Cholic Acid anilide

Cat.No: T36075

Cat.No: T36658

Cat.No: T35629

Cat.No: T36034

Cat.No: T37754

3-Acetyl Betulinaldehyde

Cat.No: T35686

Cat.No: T37414

Cat.No: T36096

Cat.No: T36215

Cat.No: T36047

Cat.No: T36046

Cat.No: T35527

Synonym: PI3Kα-IN-4

O-Desmethyl-N-deschlorobenzoyl Indomethacin

Cat.No: T36418

Cat.No: T38381

Deltorphin II (trifluoroacetate salt)

Cat.No: T36722

Cat.No: T36486

Cat.No: T36629

p38α inhibitor 2

Cat.No: T36012

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat.No: T37861

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

Guanfacine-13C,15N3

Cat.No: T35591

Synonym: Guanfacine-13C,15N3

BODIPY-aminoacetaldehyde diethyl acetal

Cat.No: T35568

Cat. No.	Product Name	Target	Signaling Pathways
T36448	(E)-Ajoene
	(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanoth...

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Cat.No: T36448

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