|
T0947
|
Dexamethasone acetate
Dexamethasone 21-acetate,醋酸地塞米松,Dexamethason acetate,NSC 39471
|
Glucocorticoid Receptor;
Mitophagy;
IL Receptor;
Annexin A;
NOS;
Antibacterial;
Autophagy |
Autophagy;
Endocrinology/Hormones;
GPCR/G Protein;
Immunology/Inflammation;
Microbiology/Virology |
|
Dexamethasone acetate (NSC 39471) 是一种糖皮质素类甾体，有抗炎和免疫抑制活性。它可研究眼部感染。 |
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T3469
|
PCI-27483
PCI27483
|
Others |
Others |
|
PCI-27483 是一种FVIIa/tissue factor 抑制剂，具有抗肿瘤的作用。 |
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TP1820L
|
Osteogenic Growth Peptide, OGP acetate
Osteogenic Growth Peptide, OGP acetate(132996-61-3 free base)
|
Others |
Others |
|
Osteogenic Growth Peptide, OGP acetate(132996-61-3 free base) 是一种短的、天然存在的 14 聚体生长因子肽，存在于血清中，浓度为 μM。成骨生长肽 OGP 是局部骨髓损伤全身成骨反应机制的关键因素。 |
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T1823
|
IOX2
IOX 2,JICL38
|
HIF/HIF Prolyl-Hydroxylase |
Chromatin/Epigenetic;
Metabolism |
|
IOX2 (IOX 2) 是特异性的脯氨酰羟化酶-2 抑制剂，IC50=22 nM。 |
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T4567
|
Sulfaphenazole
Plisulfan,Raziosulfa,Depocid,磺胺苯吡唑,Depotsulfonamide
|
P450;
Antibacterial |
Metabolism;
Microbiology/Virology |
|
Sulfaphenazole (Plisulfan) 是一种 CYP2C9的特异性抑制剂，抑制 CYP2C9介导的亚油酸动脉粥样硬化和促炎症效应，增加 AP-1的氧化应激和激活。 |
|
T12006
|
Metarrestin
ML246
|
DNA/RNA Synthesis |
Cell Cycle/Checkpoint;
DNA Damage/DNA Repair |
|
Metarrestin (ML246) 是一种口服有效的选择性核仁周区室 (PNC) 抑制剂，可有效抑制转移。Metarrestin 破坏核仁结构并抑制 RNA 聚合酶 (Pol) I 转录，部分是通过与翻译延伸因子 eEF1A2 的相互作用。 |
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T22833
|
H-9 dihydrochloride
|
EGFR;
5-HT Receptor;
PKA |
Angiogenesis;
GPCR/G Protein;
JAK/STAT signaling;
Neuroscience;
Tyrosine Kinase/Adaptors |
|
H-9 dihydrochloride 是一种具有有效性的蛋白激酶（ PKA）抑制剂。H-9 Dihydrochloride 在低浓度下显著降低 5-HT 的兴奋性反应。H-9 Dihydrochloride 会对咽部活动产生影响。H-9 Dihydrochloride 对 EGF (表皮生长因子)依赖的上皮细胞系的信号转导和细胞生长有抑制作用。 |
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T22297
|
Clindamycin hydrochloride monohydrate
Clindamycin alcoholate
|
Antibiotic |
Microbiology/Virology |
|
Clindamycin hydrochloride monohydrate（Clindamycin alcoholate）是一种口服蛋白质合成抑制剂，具有在金黄色葡萄球菌中以亚抑制浓度(sub-MICs)抑制毒力因子表达的能力。其抗性来源于50S核糖体亚基（23S rRNA）的抗生素结合位点通过酶促甲基化。此外，Clindamycin hydrochloride monohydrate能显著减少杀白细胞毒素（PVL）、毒性休克-葡萄球菌毒素（TSST-1）或α-溶血素（Hla）的产生。 |
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T76810
|
Ganitumab
AMG 479
|
IGF-1R |
Tyrosine Kinase/Adaptors |
|
Ganitumab (AMG 479) 是一种高效的1型胰岛素样生长因子受体 (IGF1R) 单克隆抗体。Ganitumab 在低浓度下识别与 IGF1R 结合，KD 值为0.22 nM，Ganitumab 对小鼠 IGF1R 与 IGF1 和 IGF2 的相互作用有抑制作用。Ganitumab 可用于研究癌症。 |
|
T14775
|
Bragsin2
6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one,Bragsin 2
|
Others |
Others |
|
Bragsin2 (6-methoxy-5-nitro-2-(trifluoromethyl)chromen-4-one) 是非竞争性的核苷酸交换因子 BRAG2选择性抑制剂，其 IC50值为 3 μM。它能够结合到 BRAG2 的 PH 结构域和磷脂双分子层的界面处，使 BRAG2 无法激活磷脂化的 Arf GTPase。它能够影响乳腺癌干细胞。 |
|
T31206
|
Darexaban
YM 150,Darexaban, Tanexaban,YM150
|
Factor Xa |
Metabolism |
|
Darexaban (Tanexaban, YM-150) 是选择性的、口服具有活力的 Xa 因子 (FXa) 抑制剂，IC50=54.6 nM。它对其他相关丝氨酸蛋白酶(如胰蛋白酶、凝血酶和激肽释放酶)具有高选择性。它具有抗凝和抗血栓形成作用。 |
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T38293
|
4-CPPC
|
Others |
Others |
|
4-CPPC 是一种巨噬细胞迁移抑制因子 2 (MIF-2; IC50= 27 μM) 的抑制剂。它对 MIF-2 的选择性高于 MIF-1 (IC50= 450 μM)。 当以 10 μM 浓度使用时，它在体外抑制 MIF-2，但不抑制 MIF-1，与 CD74 结合。 4-CPPC（5、10 和 25 μM）抑制原代人皮肤成纤维细胞中 MIF-2 诱导的 ERK1/2 磷酸化。 |
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T16500
|
PF-3450074
PF-74
|
HIV Protease |
Microbiology/Virology;
Proteases/Proteasome |
|
PF-3450074 (PF-74)是 HIV-1 衣壳蛋白的特异性抑制剂，可广谱抑制 HIV 分离株。它在 HIV-1 感染的早期阶段起作用，通过与 CPSF6 和 NUP153 的结合直接竞争来抑制病毒复制，并阻断病毒生命周期的脱膜，组装和逆转录步骤。 |
|
T0983L
|
DL-Penicillamine
3-Sulfanylvaline,DL-青霉胺
|
Antibiotic |
Microbiology/Virology |
|
DL-Penicillamine (3-Sulfanylvaline) 是一种螯合剂，推荐用于去除威尔逊病患者体内多余的铜。 它仅存在于使用或服用该药物的个体中。它是青霉素类抗生素最具特征的降解产物。它被用作抗风湿药和威尔逊病的螯合剂。 |
|
T26968
|
CCT036477
CCT 036477,CCT-036477
|
|
|
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CCT036477 is a selective inhibitor of wingless-type MMTV integration site family dependent transcription. CCT036477reduces the transcriptional activity of the T-cell factor and lymphoid enhancer factor transcription factor family at the ß-catenin level. |
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T35926
|
Bz-IEGR-pNA (acetate)
|
|
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Bz-IEGR-pNA is a colorimetric substrate for Factor Xa.1 Factor Xa preferentially binds to and cleaves the Ile-Glu-Gly-Arg (IEGR) peptide sequence to release p-nitroanilide (pNA), which can be quantified by colorimetric detection at 405 nm as a measure of Factor Xa activity.References1. Aruell, L., Friberger, P., Karlsson, G., et al. A new sensitive and highly specific chromogenic peptide substrate for factor Xa. Thromb. Res. 11(5), 595-609 (1977).
Bz-IEGR-pNA is a colorimetric substrate for Fact... |
|
T29190
|
YM-75466
YM 466,YM-466,YM75466,YM 75466,YM-75466 Free
|
|
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YM-75466 is a factor Xa inhibitor. YM-75466 did not prolong coagulation time even at the dose which exerted significant antithrombotic effects, while it decreased TAT level in plasma in a dose-dependent manner. |
|
TP1820
|
Osteogenic Growth Peptide, OGP
|
|
|
|
Osteogenic Growth Peptide, OGP is a short, naturally occurring 14-mer growth factor peptide found in serum at μM concentrations. Osteogenic growth peptide OGP is a key factor in the mechanism of the systemic osteogenic response to local bone marrow injury |
|
TP2048
|
α-Helical CRF(9-41)
α-helical CRF 9-41
|
|
|
|
Corticotropin-releasing factor receptor antagonist (Ki values are 17, 5 and 0.97 at human CRF1, rat CRF2α and mouse CRF2β receptors respectively). |
|
T37157
|
8(S)-HEPE
|
|
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8(S)-HEPE is a monohydroxy fatty acid produced by lipoxygenase oxidation of EPA. It acts to promote hatching of barnacle eggs at 10 nM, although it is not clearly identified as the natural egg hatching factor. |
|
T25888
|
NSC-670224
NSC 670224
|
|
|
|
NSC-670224 is an inhibitor of histone deacetylases-6 (HDAC6) and nuclear factor-κB (NF-κB) activation blocker. It has been shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related t |
|
T29072
|
UR-1505
UR1505,UR 1505
|
|
|
|
UR-1505 is a nuclear factor of activated T cells (NF-AT) inhibitor. UR-1505 acts by inhibiting T cell activation depending on T cell receptor signaling pathway. Furthermore, the antiproliferative effects of UR-1505 are not a consequence of decreased cell |
|
T27033
|
CKD-712
CKD 712,CKD712
|
|
|
|
CKD-712 is a nuclear factor NF-kappa B inhibitor. CKD-712 suppressed MMP-9, but not MMP-2 and other NF-κB-regulated proteins involved in cancer metastasis such as VEGF. CKD-712 induced cell cycle arrest at G2M phase by suppressing cyclin A, cyclin B and C |
|
T35818
|
CAY10669
|
|
|
|
CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro. |
|
TP1361
|
S961 TFA (1083433-49-1 free base)
S961 TFA
|
|
|
|
S961 TFA is A high affinity insulin receptor (IR) antagonist with IC50 for hir-a, hir-b and human insulin-like growth factor I receptor (higf-ir) at 0.048, 0.027 and 630 nM, respectively. |
|
T28015
|
Mequitamium iodide
LG-30435,LG 30435,LG30435
|
|
|
|
Mequitamium iodide is a platelet activating factor (PAF) inhibitor. Mequitamium inhibits PAF-acether induced platelet aggregation and bronchoconstriction. Mequitamium is capable of inhibiting platelet-mediated effects of PAF by interfering with secondary |
|
T11170
|
eIF4A3-IN-1
|
Others |
Others |
|
eIF4A3-IN-1 is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD. |
|
T36098
|
Isovaleryl-L-carnitine (chloride)
|
|
|
|
Isovaleryl-L-carnitine is a naturally occurring acylcarnitine that is formed via metabolic conversion of L-leucine. It increases survival and decreases apoptosis in hepatocyte growth factor-deprived murine C2.8 hepatocytes when used at a concentration of 1 mM. Isovaleryl-L-carnitine inhibits amino acid deprivation-induced proteolysis and autophagy in isolated perfused rat liver when used at concentrations of 77 and 100 μM, respectively. Increased levels of isovaleryl carnitine are associated wit... |
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T76908
|
Anumigilimab
|
|
|
|
Anumigilimab (CSL-324) 是一种人源化IgG2a 单抗，靶向人粒细胞集落刺激因子 (G-CSF) 受体。Anumigilimab 可用于炎症部位中性粒细胞数量增加的研究。 |
|
T60722
|
Prohibitin ligand 1
|
|
|
|
Prohibitin ligand 1 (Compound 22i) 是心脏保护剂抑制素配体， 在纳摩尔浓度下表现出体外心脏保护活性。Prohibitin ligand 1 可诱导促生存因子STAT3的磷酸化。 |
|
T36783
|
BPIQ-II (hydrochloride)
|
|
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|
BPIQ-II is a linear imidazoloquinazoline that potently inhibits the tyrosine kinase activity of the epidermal growth factor receptor (EGFR; IC50 = 8 pM). It is selective for EGFR over an assortment of other tyrosine and serine/threonine kinases. Cellular studies indicate that BPIQ-II can enter cells and very selectively shut down EGF-stimulated signal transmission by binding competitively at the ATP site of EGFR. |
|
T70170
|
Milvexian TFA
|
|
|
|
Milvexian, also known as BMS-986177 and JNJ-70033093, is a blood coagulation factor XIa inhibitor. Milvexian demonstrated good selectivity over plasma kallikreinKi = 44 nM (400-fold selective), and chymotrypsinKi = 35 nM (318-fold selective). At a dose of 1.5 mg/kg, Milvexian exhibited an overall
exposure of 1215 nM/h, low clearance of 10.3 mL/min/kg, and oral bioavailability of 32%. |
|
T35538
|
HPI-1 (hydrate)
HPI-1 hydrate
|
|
|
|
HPI-1 (hydrate) is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Sonic Hh (IC50= 1.5 μM) without significantly affecting Wnt signaling (IC50≥ 30 μM).1HPI-1 suppresses Hh activation induced by loss of Suppressor of Fused or by Gli overexpression, suggesting action at posttranslational modification of Gli protein or at the interaction of Gli with a co-factor.1HPI-1 (hydrate) also inhibits signaling through the oncogenic Smoothened (Smo) mutant SmoM2 in neuron precursors, prev... |
|
T38328
|
CU-32
|
|
|
|
CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM.
1.Padilla-Salinas... |
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T37338
|
N-3-oxo-pentanoyl-L-Homoserine lactone
|
|
|
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N-3-oxo-pentanoyl-L-Homoserine lactone is a chain-shortened derivative of the bacterial quorum sensing signaling molecule N-3-oxo-octanoyl-L-homoserine lactone .1It inhibits binding of the autoinducer N-3-oxo-hexanoyl homoserine lactone toE. colicontaining the transcription factor LuxR when used at a concentration of 230 nM.2It acts as an autoinducer to activate theV. fischeriluminescence system inE. coliwhen used at concentrations ranging from 20 to 200 nM.
1.Chhabra, S.R., Stead, P., Bainton, ... |
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T61306
|
SRI-41315
|
|
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|
SRI-41315, a chemical compound, effectively addresses premature termination codons (PTCs) associated with cystic fibrosis in immortalized and primary human bronchial epithelial cells. It induces a prolonged pause at stop codons, resulting in the restoration of cystic fibrosis transmembrane conductance regulator (CFTR) expression and function. This compound achieves PTC suppression by reducing the abundance of the termination factor eRF1. Additionally, SRI-41315 synergistically enhances CFTR acti... |
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T69555
|
XUN49524
|
|
|
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XUN49524 also known as Vezf1-IN-T4, is an inhibitor of the pro-angiogenic activity of the zinc finger transcription factor Vezf1. XUN49524 was first reported in Molecules (2018), 23(7), 1615/1-1615/15 . This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming). |
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T72928
|
CDK4/6-IN-15
|
|
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CDK4/6-IN-15 是一种口服有效和选择性 CDK4/6抑制剂。CDK4/6-IN-15 能有效抑制癌细胞生长。CDK4/6-IN-15 将细胞周期阻滞在 G1 期，并抑制视网膜母细胞瘤肿瘤抑制蛋白 (Rb) 在 S780 位点的磷酸化和 E2 因子 (E2F) 调控的基因表达。 |
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T82866
|
Biotin-PEG-Biotin (MW 20000)
|
|
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Biotin-PEG-azide (MW 2000) 为含有生物素标记的聚乙二醇 (PEG) 衍生物。该生物素（Biotin）作为酶辅因子，在蛋白质标记应用中具有重要作用，而PEG是低毒性且具亲水性的水溶性聚合物。 |
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T36523
|
Extracellular Death Factor
|
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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... |
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T36404
|
PRLX-93936
|
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PRLX-93936 is an analog of erastin that has antitumor activity. It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay). PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM... |
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T71641
|
BMS-593214
|
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BMS-593214 是一种活性位点定向因子 (F)VIIa 抑制剂。BMS-593214 具有抗血栓和抗出血特性。BMS-593214 是人 FVIIa 的直接竞争性抑制，也是 VIIa 激活底物 FX 的非竞争性抑制剂。BMS-593214 预防电诱导颈动脉血栓形成 (AT)、线诱导腔静脉血栓形成 (VT)。 |
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T38329
|
CU-76
|
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CU-76 is an inhibitor of cyclic GMP-AMP synthase (cGAS; IC50= 0.24 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. CU-76 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM.
1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP sy... |
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T68393
|
SNX-7081
|
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NX-7081 is a novel small molecule inhibitor of Hsp90, which blocks components of inflammation, including cytokine production, protein kinase activity, and angiogenic signaling. SNX-7081 showed strong binding affinity to Hsp90 and expected induction of Hsp70. NF-kappaB nuclear translocation was blocked by SNX-7081 at nanomolar concentrations, and cytokine production was potently inhibited. Growth factor activation of ERK and JNK signaling was significantly reduced by SNX-7081. NO production was a... |
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T41155
|
MS 154
|
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MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioa... |
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T36461
|
CAY10748
CAY10748
|
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CAY10748 is an agonist of stimulator of interferon genes (STING; IC50= 0.3794 μM in a competition binding assay).1It activates STING in STING-expressing, but not STING knockout, THP-1 cells (EC50s = 0.287 and >100 μM, respectively, in a reporter assay). It induces phosphorylation of STING at the serine in position 366, as well as phosphorylation of TBK1 and IFN regulatory factor 3 (IRF3), indicating activation of the STING-TBK1-IRF3 signaling pathway. CAY10748 increases the secretion of IFN-β an... |
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T36627
|
Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)
|
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Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protei... |
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T36357
|
Dimethyldioctadecylammonium (bromide)
|
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Dimethyldioctadecylammonium (DDA) is a cationic amphipathic lipid. DDA liposomes containing an Ag85B-ESAT-6 antigen induce antigen deposition at an intramuscular or subcutaneous injection site in mice, increasing immune cell exposure to the antigen. In a guinea pig model of M. tuberculosis infection, spleen bacterial load is reduced and lung and spleen lesion numbers are decreased when the mycobacterial lipid antigens Ac2SGL and PIM2 are administered in liposomes comprised of DDA and a synthetic... |
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T38045
|
Cholesterol β-D-Glucoside
|
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Cholesterol β-D-glucoside is a derivative of cholesterol that contains β-D-glucose . It is formed from cholesterol and glucosylceramide by β-glucosidase 1. It activates heat shock transcription factor 1 (Hsf1) in response to heat shock, which increases the expression of heat shock protein 70 (Hsp70) in TIG-3 human fetal lung fibroblasts when used at a concentration of 10 μM. Cholesterol β-D-glucoside (100 mg/kg) prevents ulcer formation following cold-restraint stress and increases Hsf1 activity... |
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T69323
|
Dexamethasone sodium succinate
|
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Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regul... |
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