|
T10638
|
BY27
|
Epigenetic Reader Domain |
Chromatin/Epigenetic |
|
BY27 是一种具有强效性和选择性的 BET BD2 抑制剂（Ki：3.1 nM），具有抗癌活性，抑制 BRD2、BRD3、BRD4 和 BRDT 的 BD1/BD2，抑制肿瘤生长。 |
|
T39321
|
CC-99677
CC99677,Gamcemetinib,CC 99677
|
HSP;
MAPK |
Cytoskeletal Signaling;
MAPK;
Metabolism |
|
CC-99677 (Gamcemetinib) 是一种一种用于自身免疫性疾病的选择性靶向共价MAPKAPK2(MK2)抑制剂，通过亲核芳族取代(SNAr)机制将生化效力转化为LPS活化的单核细胞THP-27细胞中热休克蛋白27(HSP1)磷酸化的有效抑制所显示的细胞效力。CC-99677 在大鼠实验中展现出在生化(IC 50 =156.3 nM)和细胞检测(EC 50 =89 nM)中均有 |
|
T38192
|
Unifiram
|
Others |
Others |
|
Unifiram 是一种认知增强剂。 Unifiram 诱导大鼠海马 CA1 区场兴奋性突触后电位 (fEPSP) 幅度的持久增加 (EC50= 27 nM) 并增加大鼠大脑皮层中乙酰胆碱 (ACh) 的释放。 |
|
TP1936L1
|
RFRP3(human) acetate(311309-27-0 free base)
|
Neuropeptide Y Receptor |
GPCR/G Protein;
Neuroscience |
|
RFRP3(human) acetate(311309-27-0 free base) 是一种人类 GnIH 肽同源物，是一种有效的促性腺激素分泌抑制剂，可抑制 Ca2+ 动员。它是一种 NPFF1 受体激动剂，它抑制毛喉素诱导的 cAMP 产生，IC50 为 0.7 nM。 |
|
T0839L
|
S-(+)-Ketoprofen
RP-19583,Dexketoprofen,(S)-(+)-Ketoprofen,(S)-Ketoprofen,(S)-(+)-酮洛芬,右旋酮洛芬
|
COX |
Immunology/Inflammation;
Neuroscience |
|
S-(+)-Ketoprofen ((S)-(+)-Ketoprofen) 抑制 COX-1和 COX-2的IC50值分别为 1.9 和 27 nM。 |
|
T24146
|
HOCPCA
|
|
|
|
HOCPCA is an effective and selective ligand for the GHB binding sites that acts by binding with 27 times better affinity than GHB itself and crossing the blood-brain barrier in vitro and in vivo. |
|
T39889
|
Antitumor agent-23
|
|
|
|
Antitumor agent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respectively. |
|
T80148
|
GRP (14-27) (human, porcine, canine)
|
Bombesin Receptor |
GPCR/G Protein |
|
GRP (14-27) (human, porcine, canine) 表现为铃蟾肽受体配体。其特异性结合受到 GTP 和 GDP 的抑制作用，但 GMP 对此无影响。 |
|
T37206
|
CCK (27-33) (non-sulfated)
|
|
|
|
CCK (27-33) is a C-terminal fragment of CCK , a peptide hormone found in the intestine and brain that stimulates digestion, mediates satiety, and is involved in anxiety. Non-sulfated CCK (27-33) inhibits binding of [3H]naloxone in rat cerebellum membranes (IC50 = 4 uM) and inhibits electrically-stimulated contraction of isolated guinea pig ileum (IC50 = 17 uM), an effect that can be reversed by naloxone. Unlike sulfated CCK (27-33), the non-sulfated form does not reduce exploratory behavior in m... |
|
T61141
|
Antitubercular agent-27
|
|
|
|
Antitubercular agent-27 (compound 1) 是一种有效的抗结核药剂，IC50值为 3.2 μM，MICb> 值为 7.8 μM，IC90值为 7.0 μM。Antitubercular agent-27 对结核分枝杆菌 H37Rv 的耐药分离株显示出抗分枝杆菌活性。Antitubercular agent-27 显示出有效的细胞内抗分枝杆菌活性和低细胞毒性。 |
|
T35590
|
Graphislactone A
|
|
|
|
Graphislactone A is an antioxidant produced by Cephalosporium IFB-E001 and M. olivacea. It exhibits dose-dependent scavenging activity against DPPH radicals and metal ion-dependent hydroxyl radicals in vitro. Graphislactone A reduces peroxidation of human LDL and slows peroxidation of linoleic acid by 4.4-fold. It also inhibits acetylcholinesterase (AChE) with an IC50 value of 27 μM. |
|
T61656
|
Antitumor agent-53
|
|
|
|
Antitumor agent-53 is a potent compound that effectively inhibits tumor growth. It achieves this by inducing cell cycle arrest at the G2/M phase and promoting apoptosis in HGC-27 cells through the inhibition of the PI3K/AKT pathway. Furthermore, Antitumor agent-53 holds promise for further research in the treatment of gastrointestinal tumors [1]. |
|
T61447
|
CXCR2 antagonist 4
|
|
|
|
CXCR2 antagonist 4 (compound 7) is a highly potent antagonist that inhibits CXCR2 with an IC50 value of 0.13 μM. It also effectively inhibits the cytosolic calcium increase induced by CXCL8, with an IC50 value of 27 μM. CXCR2 antagonist 4 shows promising potential for anticancer research [1]. |
|
T20016
|
Diuron
HW 920,Dirurol,Karmex,Lucenit,Marmer,Seduron
|
|
|
|
Diuron is a Phenylurea herbicide that inhibits photosynthesis by preventing the formation of ATP and NADH. Diuron (25 nM/ml) decreases total respiration in roots of wheat by 50% and ground respiration by 100%. Diuron (2,500 ppm, dietary) increases the inc |
|
T37654
|
5(S)-HETE lactone
|
|
|
|
5(S)-HETE lactone is a cyclic ester formed by acid-catalyzed nucleophilic addition of the C-5 hydroxyl to the C-1 carboxyl of 5(S)-HETE. The ability of (±)5-HETE lactone to inhibit rat basophilic leukemia cell 5-lipoxygenase (IC50 = 27 μM) may be entirely due to the 5(S) isomer, but the enantiomers have not been tested separately. |
|
T63952
|
GRPR antagonist-2
|
|
|
|
GRPR antagonist-2 是胃泌素释放肽受体 (GRPR) 的有效拮抗剂，对某些癌细胞具有细胞毒性（能够作用于 HGC-27 细胞 (IC50: 0.77 μM) 和 Pan02 细胞 (IC50: 2.5 μM)），表现出抗癌效果。 |
|
T80515
|
β-Endorphin (1-27) (human)
|
Opioid Receptor |
Endocrinology/Hormones;
GPCR/G Protein;
Neuroscience |
|
β-Endorphin (1-27) (human) 是一种 opioid 拮抗剂，与 μ-、δ- 及 κ-阿片受体结合，其 Kis 分别为 5.31、6.17 及 39.82 nM。该化合物还能够抑制由 β-Endorphin 及 etorphine 引起的痛觉消失。 |
|
T74945L
|
SARS-CoV-2-IN-27 disodium
|
|
|
|
SARS-CoV-2-IN-27 disodium 是具有扩展长度分子镊子的双臂二磷酸C6烷基酯。它显示出抗病毒活性，分别在抑制SARS-CoV-2活性和病毒尖刺伪粒子转导方面的IC50为1.0 μM和1.7 μM。此外，SARS-CoV-2-IN-27 disodium能引起脂质体膜破坏，其EC50为6.5 μM。 |
|
T36427
|
PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)
|
PACAP |
GPCR/G Protein |
|
Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, ... |
|
T61857
|
DNA-PK-IN-4
|
|
|
|
DNA-PK-IN-4 (WO2021209055A1, compound 27), an imidazolinone derivative compound, is a highly effective inhibitor of DNA-PK, specifically targeting DNA-PKcs activity. By inhibiting DNA-PKcs, the compound significantly impairs tumor DNA repair mechanisms and triggers apoptosis in cells. With its potential application in cancer research, DNA-PK-IN-4 holds promise for further investigation [1]. |
|
T78853
|
PI3K-IN-47
|
PI3K |
PI3K/Akt/mTOR signaling |
|
PI3K-IN-47 (Compound 27) 是一款高度选择性的二价PI3K抑制剂，对PI3Kα具有极低的半抑制浓度（IC50: 0.44 nM）, 同时对PI3Kβ、PI3Kγ、PI3Kδ也表现出良好的抑制活性（IC50分别为7.18 nM、13.92 nM、22.83 nM）。此化合物能够有效诱导细胞周期在G1期发生暂停，并且在体外抑制集落形成和细胞迁移。对于HGC-27异种移植的小鼠模型，PI3K-IN-47能够显著抑制肿瘤生长。 |
|
T38193
|
β-Endorphin (1-27) (human) (trifluoroacetate salt)
|
|
|
|
β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in ... |
|
T81182
|
Secretin (swine)
|
|
|
|
Secretin (swine)为源自猪的神经内分泌激素，由十二指肠黏膜S细胞产生，具有27个氨基酸的多肽结构，并针对分泌素受体起作用。此激素在各类成熟肠内分泌细胞亚群中表达，受脂肪酸的促进。它主要激发胰腺释放水和碳酸氢盐，同时在消化系统、中枢神经系统和能量代谢方面具有广泛应用。 |
|
T74945
|
SARS-CoV-2-IN-27
|
|
|
|
SARS-CoV-2-IN-27 为具有扩展长度的双臂二磷酸 C6 烷基酯分子镊子，显示出针对 SARS-CoV-2 的抗病毒活性。其抑制 SARS-CoV-2 活力的 IC50 为 1.0 μM，针对病毒尖刺伪粒子转导的 IC50 为 1.7 μM。此外，该化合物能引起脂质体膜破坏，其 EC50 为 6.5 μM。 |
|
T35669
|
Neuromedin C (trifluoroacetate salt)
|
|
|
|
Neuromedin C is a bombesin-like neuropeptide that stimulates uterine smooth muscle contraction and the release of gastrin , somatostatin, and amylase in rats. Neuromedin C is a truncated form of gastrin-releasing peptide corresponding to the GRP amino acids 18-27. It inhibits GRP and bombesin binding to rat pancreatic membranes (IC50s = 0.4 and 2.2 nM, respectively), which can be reduced by sodium chloride and guanylyl imidodiphosphate . Neuromedin C induces scratching and mast cell degranulatio... |
|
T21795
|
CRT5
|
|
|
|
CRT5 是一种吡嗪苯甲酰胺，对经 VEGF 处理的内皮细胞中的所有三种 PKD 亚型 (对 PKD1、PKD2 和 PKD3 的 IC50s 分别为 1、2 和 1.5 nM) 都是一种有效的选择性抑制剂，并且 CRT5 减少 VEGF 诱导的内皮细胞迁移、增殖和微管生成。 |
|
T81825
|
Melan-A/MART-1 analog
[Leu27]-Melan-A, MART-1 (26-35)
|
|
|
|
[Leu27]-Melan-A, MART-1 (26-35)是一种具有改良的HLA-A*0201结合能力和增强的免疫原性及抗原性的生物活性肽。该类似物在第27位的Leu替换了Ala，与原生Melan-A (26-35)相比表现出更佳的性能。当序列N端为谷氨酰胺(Q)或谷氨酸(E)时，肽可能会自发形成焦谷氨酰(pGlu)。Q或E到pGlu的转化是自然发生的，pGlu的疏水性γ-内酰胺环被认为可增强针对胃肠道蛋白酶的抵抗力，使得含pGlu的肽成为这类肽的正常子集，在HPLC分析中通常作为评估肽纯度的一部分。 |
|
T35659
|
3'-Dephosphocoenzyme A
|
|
|
|
3'-Dephosphocoenzyme A is an intermediate in the biosynthesis of coenzyme A from pantothenic acid .1 It is phosphorylated by CoA synthase in humans to form CoA. 3'-Dephosphocoenzyme A can be used as a transcription initiator in the synthesis of CoA-RNA by in vitro transcription.2,3
References1. Leonardi, R., Zhang, Y.M., Rock, C.O., et al. Coenzyme A: Back in action. Prog. Lipid Res. 44(2-3), 125-153 (2005).2. Huang, F. Efficient incorporation of CoA, NAD and FAD into RNA by in vitro transcripti... |
|
T37732
|
AMG 21629
|
|
|
|
Potent and selective TRPV1 antagonist. Blocks Ca2+ uptake by CHO cells expressing TRPV1 receptors and acid-induced Ca2+ uptake, respectively). Exhibits >4000-fold selectivity for TRPV1 over other TRP channels. Blocks capsaicin-induced flinch response and causes hyperthermia in rats. Orally available and non-CNS penetrant.
Tamayo et al (2008) Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists. J.Med.Chem. 51 2744 PMID:18386885 |Gavva et al... |
|
T38123
|
5(6)-Carboxy-2′,7′-dichlorofluorescein diacetate
|
|
|
|
5(6)-Carboxy-2’,7’-dichlorofluorescein diacetate is an oxidant-sensitive and cell-permeable fluorescent probe.1Base hydrolysis of the ester bonds by intracellular esterases releases the acetate groups and the resulting compound, 5(6)-carboxy-2’,7’,-dichlorofluorescein, is oxidized by reactive oxygen species (ROS) and nitric oxide (NO) and displays excitation/emission maxima of 504 and 530 nm, respectively, which can be quantified as a measure of oxidant production.
1.Hempel, S.L., Buettner, G.R.... |
|
T36676
|
Rineterkib hydrochloride
|
|
|
|
Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1].
ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C... |
|
T36409
|
Roccellic Acid
|
|
|
|
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.1,2 It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 μg/ml for both).1 Roccellic acid (100 μg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.2
|1. Sweidan, A., Chollet-Krugler, M., Sauvager, A., et al. Antibacterial activities of natural lichen compounds against Streptococcus ... |
|
T36851
|
Peptide5
|
|
|
|
Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain.
O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats.... |
|
T37018
|
OH-Chol
|
|
|
|
OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intrat... |
|
T37044
|
1,2-Dioleoyl-rac-glycerol-13C3
1,2-Dioleoyl-rac-glycerol-13C3
|
|
|
|
1,2-Dioleoyl-rac-glycerol-13C3 is intended for use as an internal standard for the quantification of 1,2-dioleoyl-rac-glycerol by GC- or LC-MS. 1,2-dioleoyl-rac-glycerol is a diacylglycerol that contains oleic acid at the sn-1 and sn-2 positions. It effectively binds the C1 domain to activate conventional protein kinase C forms and serves as a substrate for diacylglycerol kinases and multisubstrate lipid kinase.1,2,3
|1. Yamaguchi, Y., Shirai, Y., Matsubara, T., et al. Phosphorylation and up-reg... |
|
T36894
|
5-Bromouridine
|
|
|
|
5-Bromouridine is a brominated analog of the nucleoside uridine .1It can be incorporated into RNA and subsequently detected by antibodies against bromodeoxyuridine .25-Bromouridine decreases the viability of HL-60 and MOLT-4 cells (LC50s = 10 and 20 μM, respectively). It induces apoptosis and halts the cell cycle at the S phase in HL-60 cells. It is photoreactive, and UV irradiation has been used to cross-link RNA containing 5-bromouridine to proteins in the study of of RNA-protein interactions.... |
|
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... |
|
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... |
|
T35772
|
Emestrin
|
|
|
|
Emestrin is a mycotoxin originally isolated from E. striata that has antimicrobial, immunomodulatory, and cytotoxic activities.1,2,3,4,5 It is active against the fungi C. albicans and C. neoformans, as well as the bacteria E. coli, S. aureus, and methicillin-resistant S. aureus (MRSA; IC50s = 3.94, 0.6, 2.21, 4.55, and 2.21 μg/ml, respectively).2 Emestrin is a chemokine (C-C motif) receptor 2 (CCR2) antagonist (IC50 = 5.4 μM in a radioligand binding assay using isolated human monocytes).3 Emestr... |
|
T37741
|
N-hexadecanoyl-L-Homoserine lactone
C16-HSL,N-palmitoyl-L-Homoserine,N-hexadecanoyl-L-Homoserine lactone
|
|
|
|
Quorum sensing is a regulatory system used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of which... |
|
T37736
|
N-cis-hexadec-9Z-enoyl-L-Homoserine lactone
N-(2-oxotetrahydrofuran-3S-yl) Palmitoleyl Amide,N-cis-hexadec-9Z-enoyl-L-Homoserine lactone
|
|
|
|
Quorum sensing is a regulatory process used by bacteria for controlling gene expression in response to increasing cell density.[1] This regulatory process manifests itself with a variety of phenotypes including biofilm formation and virulence factor production.[2] Coordinated gene expression is achieved by the production, release, and detection of small diffusible signal molecules called autoinducers. The N-acylated homoserine lactones (AHLs) comprise one such class of autoinducers, each of whic... |
|
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... |
|
T35597
|
Neuromedin U-23 (rat) (trifluoroacetate salt)
|
|
|
|
Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body ... |
沪公网安备 31010602006700号