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Advanced Glycation End Products
CYP19A1
Decarboxylase
DprE1
Fer/FerT kinase
Platelet aggregation
Progesterone Receptor
Others
信号通路
其他
Others
Others
Targetmol为生命科学及医药领域的科研人员提供其他未细分细胞信号通路相关产品,包括抑制剂、激动剂、调节剂、降解剂等。
HIT212063476
N-Fmoc-8-aminooctanoic acid
T71972
126631-93-4
N-Fmoc-8-aminooctanoic acid can be used as a PROTAC linker in the synthesis of PROTACs. N-Fmoc-8-aminooctanoic acid is an alkane chian with terminal Fmoc-protected amine and carboxylic acid groups. The Fmoc group can be deprotected under basic condition to obtain the free amine which can be used for further conjugations. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond.
Others
PROTAC Linker
HIT212005486
Esoxybutynin Chloride
T71889
230949-16-3
Esoxybutynin Chloride is (S)-enantiomer of oxybutynin. Esoxybutynin Chloride exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.
AChR
Others
HIT217588467
Caramiphen hydrochloride
T71107
125-85-9
Caramiphen hydrochloride is the salt form of Caramiphne (free base), which is an antimuscarinic and anticholinergic agent. It acts as an antagonist of NMDA receptor.
AChR
Others
HIT212023356
MDL-74156
T71064
127951-99-9
MDL-74156 is an active metabolite of dolasetron and a 5-hydroxy-tryptamine3 (5-HT3) antagonist.
5-HT Receptor
AChR
Others
HIT217588478
Nanatinostat TFA
T71110
1256448-48-2
Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.
Apoptosis
HDAC
Others
HIT217588017
C1A
T71602
1021463-02-4
C1A is an inhibitor of HDAC6 which modulates downstream autophagy substrates and leads to growth inhibition of a diverse set of cancer cell lines.
Apoptosis
HDAC
Others
Sirtuin
HIT218852243
Gepotidacin hydrochloride
T71490
1075235-46-9
Gepotidacin hydrochloride, also known as GSK-2140944 hydrochloride, is a potent Type II DNA topoisomerase inhibitor. Gepotidacin hydrochloride is a novel antibacterial drug candidate. Gepotidacin hydrochloride Demonstrates Absence of Fluoroquinolone-Like Arthropathy in Juvenile Rats. Gepotidacin hydrochloride is efficacious in a nonhuman primate model of pneumonic plague. When tested against Gram-negative (n = 333) and Gram-positive (n = 225) anaerobes by agar dilution, Gepotidacin hydrochloride inhibited 90% of isolates at concentrations of 4 and 2 μg/mL, respectively.
Antibacterial
Antibiotic
Others
Topoisomerase
HIT212731451
Lobaric acid
T71811
522-53-2
Lobaric acid is a depsidone metabolite that has been isolated from Stereocaulon lichen species with antioxidant, antiproliferative, antiviral, and enzyme inhibitory activites. It scavenges superoxide radicals in a cell-free assay (IC50 = 97.9 μmol) and inhibits proliferation in a panel of leukemia, colorectal, gastric, breast, ovarian, prostate, pancreatic, and lung cancer cell lines (EC50s = 15.2-63.9 μg/ml). Lobaric acid inhibits protein tyrosine phosphatase 1B (PTP1B; IC50 = 0.87 μM for the human recombinant enzyme) and production of 12(S)-HETE (Item No. 34570) by 12(S)-lipoxygenase (IC50 = 28.5 μM). In vivo, lobaric acid (250 μM) decreases lesion number, but not lesion diameter, in tobacco leaves infected with tobacco mosaic virus (TMV).
Lipoxygenase
Others
Phosphatase
TMV
HIT212080396
RK-20448
T71819
479501-40-1
RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2. It also inhibits BLK, Csk, Fyn, and Lyn. RK-20448 is the cis isomer of A-419259
Others
Src
Tie-2
VEGFR
HIT101587584
D-Pyrohomoglutamic Acid
T71769
72002-30-3
D-Pyrohomoglutamic acid is a building block. It has been used in the synthesis of immunoproteasome low molecular mass polypeptide 2 (LMP2) subunit inhibitors and is a component of substance P peptide analogs.
Endogenous Metabolite
Others
HIT217586292
2-Nitrophenyl a-D-glucopyranoside
T74725
56193-44-3
2-Nitrophenyl a-D-glucopyranoside 是一种 β-葡萄糖苷酶的底物。
Glucosidase
glycosidase
Others
HIT105727852
Angiogenesis inhibitor BT2
T71722
922029-50-3
Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB/ΔFosB, VCAM-1, and many genes involved in proliferation, migration, angiogenesis, and inflammation, interacting with MEK1, suppressing retinal CD31, pERK, VCAM-1, and VEGF-A165 expression.
ERK
Others
HIT215519260
AZD 1775 Linker Conjugate 1 TFA
T77496L
2858813-30-4
AZD 1775 Linker Conjugate 1 TFA 是一种参与泛素酶靶向嵌合体实验的化合物。
Others
Wee1
HIT104390701
MAC-5576
T71895
219929-01-8
MAC-5576 a SARS-CoV-2 Protease inhibitor (IC50 = 81 nM).
Others
SARS-CoV
HIT218852269
Indacaterol xinafoate
T71658
1000160-97-3
Indacaterol xinafoate is an ultra-long-acting beta-adrenoceptor agonist.
Adrenergic Receptor
Others
HIT217592482
MOTS-c
T77782
1627580-64-6
MOTS-c为源于线粒体的多肽(MDP),它通过激活AMPK途径并抑制MAP激酶-c-fos信号通路,具有抗损伤和抗炎效应。
Apoptosis
Others
HIT213887223
Vinflunine
T7594
162652-95-1
Vinflunine is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.
Microtubule Associated
Others
HIT100945709
O-allylvanillin
T78068
22280-95-1
O-allylvanillin为o-烯丙基查尔酮衍生物,呈现抗癌活性。该化合物对THP-1、HL60、Hep-G2、MCF-7细胞系生长抑制作用显著,其IC50值依次为74.76 μM、63.52 μM、90.99 μM、90.11 μM。
Endogenous Metabolite
Others
HIT214308926
Sucrose octasulfate sodium
T81074
74135-10-7
Sucrose octasulfate为硫糖铝组分,能直接刺激胃粘膜D细胞以促进生长抑素样免疫反应(SLI)的释放,进而发挥内源性胃生长抑素的溃疡愈合功能,适用于抗胃溃疡研究。
Others
Somatostatin
HIT217583936
Nocarimidazole A
T81660
1818218-33-5
Nocarimidazole A,一种来源于海洋放线菌Nocardiopsis的白色无定形固体生物碱,具紫外线活性。
Endogenous Metabolite
Others
HIT217583578
Embramine hydrochloride
T82476
13977-28-1
Embramine (hydrochloride) 为具有抗组胺及抗胆碱能特性的单乙醇胺类化合物。
Histamine Receptor
Others
HIT217583543
Human enteropeptidase-IN-3
T82163
1958037-36-9
Human enteropeptidase-IN-3是一种肽类酶抑制剂,主要作用于肠肽酶,具有长效抑制功能。该化合物广泛应用于研究肠道消化相关疾病。
Enteropeptidase (EP)
Others
HIT213945722
Indoramin hydrochloride
T82072
38821-52-2
Indoramin (hydrochloride) is a novel antihypertensive agent that exhibits selectivity for the α1A-adrenergic receptor.
Adrenergic Receptor
Others
HIT217583657
AP-C3
T82991
682795-78-4
AP-C3为cGMP依赖性蛋白激酶II (cGKII) 的有效抑制剂,其pIC50值为6.3。该化合物仅对cGKII依赖性阴离子分泌表现出微弱的抑制作用。
Others
PKA
HIT217583644
ATUX-1215
T82938
2910929-53-0
ATUX-1215是一种蛋白磷酸酶 2A (PP2A)的激活剂,能够在BLM治疗的动物模型中降低ERK、p38、JNK和Akt的磷酸化及IL-12p70、GM-CSF与IL1α的分泌,从而有助于减缓肺纤维化的发展。
Others
Phosphatase
HIT217583659
AP-C1
T82992
2234280-26-1
AP-C1是一种针对cGMP依赖性蛋白激酶II (cGKII) 的有效抑制剂,具有pIC50值为6.5。此化合物对cGKII所介导的阴离子分泌仅表现出微弱的抑制作用。
Others
PKA
HIT217583638
Biotin-hexanamide-(L-Thyroxine)
T82879
2278192-78-0
Biotin-hexanamide-(L-Thyroxine)为生物素化L-Thyroxine化合物。该化合物中的L-Thyroxine(即Levothyroxine;T4)作为一种合成甲状腺激素,广泛用于甲状腺功能减退症的研究中。
Others
Thyroid hormone receptor(THR)
HIT218832649
(±)9(10)-DiHOME
T84633
263399-34-4
(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.
DNA/RNA Synthesis
NF-κB
Others
PPAR
HIT218850491
PDHK-IN-7
T88769
1220965-73-0
PDHK-IN-7(compound 32)作为丙酮酸脱氢酶激酶抑制剂,展示了17 nM的IC50值。此化合物可在大鼠肝脏中激活PDH,且对Zucker肥胖大鼠显现出降糖效果。
Dehydrogenase
Others
HIT102599635
VU 0546110
T83960
1421523-00-3
VU 0546110 是一种针对精子特异性钾通道 SLO3 的选择性抑制剂(IC50= 64 μM),相较于 SLO1 显示出 40 倍的选择性。它能完全阻断异源性 SLO3 电流和内源性 K+ 电流。VU 0546110 抑制精子超极化并阻止其超活跃移动。
Others
Potassium Channel
HIT218832592
Prostaglandin F1β
T84530
10164-73-5
PGF1β, a biochemical compound, functions as a pivotal mediator in inflammatory processes and plays an integral role in uterine contractions. It exhibits significant regulatory effects on platelet aggregation and vasodilation, demonstrating its critical importance in cardiovascular health. Additionally, PGF1β contributes to the regulation of kidney function and electrolyte balance, illustrating its widespread impact across various physiological systems.
Others
Prostaglandin Receptor
HIT218850263
6-Bnz-5'-AMP
T88526
40871-55-4
6-Bnz-5'-AMP,一种adenosine-5'-O-monophosphate的亲脂类似物,也可能是N6-Benzoyl-cAMP的代谢产物。在烟草和大豆的组织培养中,此化合物显示出细胞分裂素的活性效应。
Endogenous Metabolite
Others
HIT218848285
Hydroxy-PP
T86696
833481-60-0
Hydroxy-PP是一种有效的CBR1抑制剂,IC50值为0.78 μM,同时有效抑制细胞质酪氨酸激酶Fyn,IC50值为5 nM。
Others
Src
HIT106502102
DJ-1-IN-1
T88153
797780-71-3
DJ-1-IN-1 (compound 797780-71-3) 作为一种有效的DJ-1抑制剂,在ACHN细胞中展示出了明显的抗增殖特性,其IC50达到了12.18 μM。此外,该化合物还能够抑制Wnt信号通路,因而在癌症研究领域具有应用潜力。
Others
Wnt/beta-catenin
HIT218849166
3-deoxy-3-fluoro-β-D-Ribofuranose 25
T87696
1884324-98-4
Compound 25 (β-D-Ribofuranose, 3-deoxy-3-fluoro-, 1,2-diacetate 5-(4-methylbenzoate)) 显示出显著的肿瘤细胞生长抑制效果。
Nucleoside Antimetabolite/Analog
Others
HIT218847721
CHI3L1-IN-1
T86048
2982256-78-8
CHI3L1-IN-1 (Compound 30),作为CHI3L1(YKL-40)的抑制剂,具有 50 nM 的IC50值。此外,该化合物还可抑制hERG通道,其IC50为 2.3 μM。
glycosidase
Others
Potassium Channel
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