|
T4277
|
Osilodrostat
LCI699
|
Glucocorticoid Receptor;
Others;
Hydroxylase |
Endocrinology/Hormones;
Metabolism;
Others |
|
Osilodrostat (LCI699) 是一种有效的人11β-羟化酶和醛固酮合成酶抑制剂，IC50分别值为2.5 和0.7nM。 |
|
T8458
|
CNQX disodium
|
iGluR |
Membrane transporter/Ion channel;
Neuroscience |
|
CNQX disodium 是一种有效的、竞争性的 AMPA /海藻酸酯受体 (AMPA/kainate receptor) 拮抗剂，IC50分别为 0.3 μM 和 1.5 μM。它能够阻止大鼠恐惧增强的表达，是一种竞争性的非 NMDA 受体拮抗剂。 |
|
T31425
|
Dibenz[a,h]anthracene
CCRIS 208,二苯葸,NSC 22433,AI3-18996,DB(a,h)A
|
DNA |
DNA Damage/DNA Repair |
|
Dibenz[a,h]anthracene (CCRIS 208) 诱导细菌DNA 损伤和基因突变，并在几种哺乳动物细胞培养物中诱导基因突变和转化。 |
|
T21012
|
Diflufenican
M&B 38544,吡氟草胺
|
Others |
Others |
|
Diflufenican (M&B 38544) 是一种选择性除草剂，用于专门防治某些阔叶杂草。 |
|
T60086
|
TTBK1-IN-2
N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
|
Microtubule Associated |
Cytoskeletal Signaling |
|
TTBK1-IN-2 (N-[4-(4-chlorophenoxy)phenyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine) 是 Tau-Tubulin 激酶 (TTBK1) 的抑制剂，IC50 为 0.24 和 4.22 µM。 TTBK1-IN-2 降低细胞培养物和转基因 TDP-43 小鼠脊髓中的 TDP-43 磷酸化。 |
|
T3031
|
A 83-01
ALK5 Inhibitor IV,A8301
|
ALK;
TGF-beta/Smad |
Angiogenesis;
Stem Cells;
Tyrosine Kinase/Adaptors |
|
A 83-01 (ALK5 Inhibitor IV) 是一种 TGF-βI 型受体 ALK5、ALK4 和 ALK7 的抑制剂 (IC50=12/45/7.5 nM)。A 83-01 可促进小鼠成纤维细胞重编程为 iPSCs。A 83-01 可用于类器官培养。 |
|
T3486
|
3-MATIDA
|
GluR;
NMDAR |
Neuroscience |
|
3-MATIDA 是一种有效的 mGluR-1 拮抗剂（IC50：6.3 μM，大鼠 mGluR-1a）。显示出 ≥ 40 倍于其他受体的选择性：mGluR-5、mGluR-2、mGluR-4 (mGluR-4a) (IC50 > 300 μM)、NMDA 和 GluR (AMPA) (IC50 = 250 μM)。 3-MATIDA 在体外培养的鼠皮质细胞和大鼠海马切片培养物中充当神经保护剂。 |
|
T60197
|
UNC 1025
|
Others |
Others |
|
UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 ... |
|
T26684
|
Auten-99 HBr
Auten-99,Auten-99 hydrochloride. Auten-99 HBr,Auten99,Auten 99
|
Phosphatase |
Metabolism |
|
Auten-99 HBr (Auten-99) 是新型肌管蛋白磷酸酶 Jumpy( MTMR14) 的抑制剂，可通过血脑屏障，具有强大的神经保护作用。 |
|
T37742
|
N-hexanoyl-DL-Homoserine lactone
C6-HSL
|
Antibiotic |
Microbiology/Virology |
|
N-hexanoyl-DL-Homoserine lactone (C6-HSL) 是从双壳类幼虫培养物中分离出来的，可降解细菌，可抑制植物病原真菌 B. cinerea 诱导的病变。N-hexanoyl-DL-Homoserine lactone 参与细菌间的N-酰基-高丝氨酸内酯 （AHL） 群体感应 （QS） 系统。 |
|
T6202
|
DAPT
LY-374973,GSI-IX
|
Apoptosis;
Beta Amyloid;
Gamma-secretase;
Autophagy |
Apoptosis;
Autophagy;
Neuroscience;
Proteases/Proteasome;
Stem Cells |
|
DAPT (LY-374973) 是一种 γ 分泌酶抑制剂，抑制总 Aβ 和 Aβ42 (IC50=115/200 nM)，具有口服活性。DAPT 也是一种 Notch 抑制剂。DAPT 可以诱导细胞分化、诱导细胞自噬和凋亡。 |
|
T32836
|
Lochnericine
|
Others |
Others |
|
Lochnericine is a alkaloid isolated from elicited cell cultures of Catharanthus roseus. |
|
T25762
|
Lucimycin
FI1163,Antibiotic 1163 F.I.,FI 1163,FI-1163,NSC 143257
|
Others |
Others |
|
Lucimycin is a macrolide antibiotic from cultures of Streptomyces lucensis. |
|
T25699
|
Levorin
Levorinum,Levorina,Levorine
|
Others |
Others |
|
Levorin is a polyene series antibiotic, obtained from cultures of Actinomyces levoris. |
|
T41140
|
Eesperamicin A1
Eesperamicin A1
|
Others |
Others |
|
Esperamicin A1, an exceedingly potent antitumor antibiotic, is derived from Actinomadura verrucosospora cultures. This compound plays a crucial role in antitumor research. |
|
T30767
|
CB-181963
CB 181963,CB181963,UNII-6784994L0W,CAB 175
|
Others |
Others |
|
CB-181963, a new cephalosporin, is an effective antistaphylococcal drug, showing excellent activity against the resistance of MRSA strains to other cephalosporins in planktonic and biofilm cultures. |
|
T85273
|
Gonadorelin acetate
|
Others |
Others |
|
Gonadorelin, a gonadotropin-releasing hormone receptor (GNRHR; Ki= 13 nM in CHO cells expressing the human receptor) agonist and tropic hormone, effectively stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from rat anterior pituitary cultures at 0.1 μg doses. Additionally, it triggers LH release from bovine anterior pituitary cultures at a 1 μM concentration. In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (ED50= 610.3 ng/kg). ... |
|
T20661
|
Tulobuterol
|
Others |
Others |
|
Tulobuterol is mainly used for the prevention and treatment of bronchial asthma, asthmatic bronchitis and chronic bronchitis. Research shows that it could inhibit rhinovirus infection in primary cultures of human tracheal epithelial cells. |
|
T33858
|
PACA
N-Propargyl Caffeamide
|
Others |
Others |
|
PACA, (N-propargyl Caffeamide)enhances NGF-induced neurite growth and reduces 6-hydroxydopamine neurotoxicity in neuron cultures. Parkinson's disease (PD) is associated with insufficient production of nerve growth factor (NGF). |
|
T84533
|
Hypogeic acid
|
Others |
Others |
|
Hypogeic acid 可从与生物滤器中硫酸盐积聚相关的自养型细菌培养物中分离得到。 |
|
T69205
|
GGTI-2166
|
Others |
Others |
|
GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells. |
|
T36401
|
DCVC
|
Others |
Others |
|
DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue p... |
|
T36852
|
Phalloidin-AMCA Conjugate
|
|
|
|
Phalloidin-AMCA conjugate is a blue fluorophore that specifically labels filamentous actin (F-actin). It consists of aminomethylcoumarin (AMCA; ex/em max = 350/450 nm) conjugated with phalloidin , a mycotoxin that binds F-actin. Phalloidin-AMCA conjugate is used in fixed and permeabilized tissue sections, cell cultures, or cell-free experiments. |
|
T11482
|
GSK2245035
|
Others |
Others |
|
GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood |
|
T68758
|
UNC10112785
|
Others |
Others |
|
UNC10112785 is a novel potent inhibitor of CDK8, CDK19, and CDK9 with IC50 at 1.05, 2.67, and 19.9 nM, respectively, causing MYC loss through both transcriptional and posttranslational mechanisms, and suppressing PDAC anchorage-dependent and anchorage-independent growth, inducing the substantial loss of MYC protein in both two-dimensional (2D) and 3D cell cultures. |
|
T37162
|
8-hydroxy Efavirenz
|
Others |
Others |
|
8-hydroxy Efavirenz is a major oxidative metabolite of the non-nucleoside reverse transcriptase inhibitor efavirenz . 8-hydroxy Efavirenz is formed when efavirenz is metabolized by the cytochrome P450 (CYP) isoform CYP2B6. It induces apoptosis in rat primary hippocampal neurons and loss of dendritic spines in rat primary hippocampal neuronal cultures when used at a concentration of 0.01 μM. |
|
T36523
|
Extracellular Death Factor
|
|
|
|
Programmed cell death in bacteria is dependent on a system of cell-to-cell communication termed quorum sensing. Extracellular death factor (EDF) is a linear pentapeptide that communicating cells produce and release, which upon reaching a sufficient concentration activates the cell death pathway in a subset of cells. It is sensitive to extreme pH, high temperatures, and other stressful conditions. At 2.5 ng/ml, EDF has been shown to facilitate mazEF-mediated cell death, significantly reducing pop... |
|
T37390
|
NS 6740
|
Others |
Others |
|
High affinity α7 nAChR partial agonist (Ki = 1.1 nM in rat; Emax < 10% of the response to ACh in rat and human). Inhibits ACh (IC50 = 2.7 nM) at α7 nAChR. Reduces LPS-induced TNF-α release from microglia enriched cultures. Anti-inflammatory.
Briggs et al (2009) Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors. Br.J.Pharmacol. 158 1486 PMID:19845675 |Thomsen et al (2012) The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS674... |
|
T29161
|
STOCK2S-26016
WNK IN B,WNK-IN-B,Compound B
|
Others |
Others |
|
WNK-IN-B is an inhibitor of Wnk signalling. WNK-IN-B is a cell-permeable diaminoacridine derivative that targets the CCT domain of SPAK and OSR1 via reversible binding. WNK-IN-B selectively suppress hypotonic shock-induced WNK signaling pathway activation |
|
T33808
|
12-Oxo phytodienoic acid
12-Oxo-Phytodienoic acid,12-OPDA,12-oxo PDA,OPDA
|
Others |
Others |
|
12-Oxo phytodienoic acid (12-oxo PDA) 是具有生物活性的 7-epi jasmonic acid 的直接前体。12-Oxo phytodienoic acid 在介导对病原体和害虫的抗性中起非依赖性作用。 |
|
T9660
|
Bexlosteride
|
Others |
Others |
|
Bexlosteride (LY300502) 是一种苯并喹啉酮类人 I 型 5α-还原酶抑制剂。Bexlosteride 在 LNCaP 细胞培养物中显示出代谢抑制、抗增殖和抗分泌作用。Bexlosteride 可用于前列腺癌的研究。 |
|
T61574
|
PD-L1-IN-1
|
Others |
Others |
|
PD-L1-IN-1, a powerful PD-L1 inhibitor, demonstrated an IC50 of 115 nM. By forming a robust bond with the PD-L1 protein, PD-L1-IN-1 effectively suppressed tumor growth by enhancing the antitumor immune activity of peripheral blood mononuclear cells in co-cultures with PD-L1 expressing cancer cells (PC9 and HCC827 cells). It significantly elevated the release of interferon γ and induced apoptosis in cancer cells, while exhibiting minimal cytotoxicity in healthy cells [1]. |
|
T37409
|
DPC-AJ1951 (trifluoroacetate salt)
DPC-AJ1951 (trifluoroacetate salt)
|
Others |
Others |
|
DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants... |
|
T35542
|
LLP-3
|
Others |
Others |
|
Survivin (also known as baculoviral IAP repeat-containing protein 5 (BIRC5)) is a member of the inhibitor of apoptosis (IAP) family that interacts with and inhibits the apoptotic function of several proteins. LLP-3 is a cell-permeable ligand of Survivin that blocks its interaction with Ran, resulting in the induction of apoptosis (IAP) in glioma stem cells (IC50 = 31 μM). It abolishes the growth of glioblastoma multiforme cell in spheres and in tumor slice cultures. |
|
T78690
|
MAO-B-IN-18
|
Monoamine Oxidase |
Neuroscience |
|
MAO-B-IN-18是高效的选择性MAO-B抑制剂，其IC50值针对hMAO-B为52 nM，对hMAO-A则为14 μM。此外，MAO-B-IN-18能显著保护神经母细胞瘤和星形胶质细胞培养物免受过氧化氢损伤。 |
|
T82373
|
FPR2 agonist 3
|
Others |
Others |
|
FPR2 agonist 3 能够抑制 LPS 刺激下的培养物中乳酸脱氢酶的释放，并减少促炎性因子IL-1β和IL-6的表达水平。此外，FPR2 agonist 3 还可以通过作用于 STAT3/SOCS3 信号通路来降低 STAT3 的磷酸化水平。 |
|
T60620
|
UCSF686
|
Others |
Others |
|
UCSF686 是一种 UCSF678 类似物，不具有 5-HT5A 效力，同时保留了脱靶亲和力（5-HT1A、5-HT2B 和 5-HT7）。 当使用 UCSF678 探测培养物和体内的 5-HT5A 依赖性活性时，建议将 UCSF686 作为对照化合物 [1]。 |
|
T69035
|
Camostat free base
|
Others |
Others |
|
Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces... |
|
T71361
|
CHS-828 nicotinate
|
Others |
Others |
|
CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, ... |
|
T69806
|
EGIS-8332
|
Others |
Others |
|
EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimenta... |
|
T38279
|
C2-8
C2-8
|
Others |
Others |
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s = 25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2... |
|
T69888
|
SB02024
|
Others |
Others |
|
SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity... |
|
T68875
|
Xylocydine
|
Others |
Others |
|
Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause... |
|
T38073
|
Thiocarlide
Isoxyl
|
Others |
Others |
|
Thiocarlide (isoxyl) is a thiourea derivative that was used in the 1960s to successfully treat tuberculosis (TB). It has considerable antimycobacterial activity in vitro and is effective against multi-drug resistant strains of Mycobacterium tuberculosis in the range of 1-10 µg/ml. [1] [2] At concentrations of 10 µM, isoxyl inhibits the synthesis of M. bovis during six hours of exposure which is similar to isoniazid (INH) and ethionamide (ETH), two other predominant anti-tuberculosis drug... |
|
T27768
|
L-696229
L696,229,L-696,229,L 696229,L696229,L 696,229
|
Others |
Others |
|
L-696229 is a specific inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT). L-696229 inhibited RT activity in a mutually exclusive manner with respect to either phosphonoformate or azidothymidine triphosphate and was a weak |
|
T83726
|
Tat-βsyn-degron TFA
|
|
|
|
Tat-βsyn-degron是一种降低α-synuclein表达的肽。其结构包括HIV-1 Tat质膜跨导域、与β-synuclein氨基酸36-45相对应的α-synuclein结合域βsyn，以及蛋白酶体定向域degron。Tat-βsyn-degron能够与重组α-synuclein结合，并在大鼠初级皮质神经元培养中降低α-synuclein水平。 |
|
T21783
|
AG-183
|
Others |
Others |
|
(Z)-Tyrphostin A51 是 Lanoconazole A51 的 Z 构型形式。Tyrphostin A51 是一种有效的蛋白酪氨酸激酶 (PTK)抑制剂，以剂量依赖性方式抑制原代星形胶质细胞培养物中 [3H]牛磺酸的体积敏感释放。Tyrphostin A51 显着降低细胞酪氨酰磷酸化水平。Tyrphostin A51 抑制基础和 EGF 诱导的人骨细胞增殖。 |
|
T36232
|
20-carboxy Arachidonic Acid
|
Others |
Others |
|
20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-A... |
|
T71651
|
GSK1370319A
|
Others |
Others |
|
GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-relate... |
|
T35558
|
KAAD-Cyclopamine
|
Others |
Others |
|
Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated onco... |
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