49
5
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8773 |
MID-1
|
Others; IGF-1R | Others; Tyrosine Kinase/Adaptors |
MID-1 是 MG53-IRS-1 相互作用的抑制剂,能够破坏 MG53 与 IRS-1 的分子缔合,并消除 MG53 诱导的 IRS-1 泛素化和骨骼肌降解,升高 IRS-1 表达水平,增加胰岛素信号传导和葡萄糖摄取。 | |||
T8955 |
PCNA-I1
|
Others | Others |
PCNA-I1 是PCNA(增殖细胞核抗原)抑制剂。它能够直接与 PCNA 三聚体结合(Kd:0.41 μM),在体内外均表现出抗肿瘤活性。 | |||
T22195 |
CBFβ Inhibitor
5-乙基-4-(4-甲氧基苯基)-1,3-噻唑-2-胺,5-Ethyl-4-(4-methoxy-phenyl)-thiazol-2-ylamine |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
CBFβ Inhibitor (5-Ethyl-4-(4-methoxy-phenyl)-thiazol-2-ylamine) 是一种细胞渗透性 CBFβ 抑制剂,可抑制其与 Runx1 的结合。 | |||
T8774 |
MS7972
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
MS7972 是一种小分子,能阻断人 p53 和 CREB 结合。它在50 μM 的时候几乎可以完全阻断 BRD 的相互作用。 | |||
TP1777L |
p2Ca acetate(142606-55-1 free base)
|
Others | Others |
p2Ca acetate(142606-55-1 free base) 是一种天然加工的肽,来源于普遍存在的酶 α-酮戊二酸脱氢酶,并被 CTL 克隆 (2C) 识别为与 I 类 MHC 蛋白 Ld 结合。 | |||
TP1313L |
Cecropin B acetate
Cecropin B acetate(80451-05-4 Free base) |
P450; Retinoid Receptor; Parasite | Metabolism; Microbiology/Virology |
Cecropin B acetate 通过破坏 PXR/类视黄醇 X 受体 α (RXR-α) 复合物与 DNA 序列的结合来诱导 NF-κB 活化并抑制 CYP3A29。 Cecropin B acetate 具有很强的抗菌活性。 | |||
T26357 |
Pitstop 2
|
Apoptosis | Apoptosis |
Pitstop2 是一种选择性的两性蛋白结合的网格蛋白末端结构域抑制剂,IC50 值为 12 μM。 Pitstop2 严重干扰受体介导的内吞作用、HIV 进入和突触小泡循环。 | |||
T11728 |
JR-AB2-011
|
mTOR | PI3K/Akt/mTOR signaling |
JR-AB2-011 是一种选择性 mTORC2抑制剂,IC50值为 0.36 μM。JR-AB2-011 通过阻断 Rictor-mTOR 联合体 (Ki: 0.19 μM) 抑制 mTORC2 活性,并且具有抗多形性胶质母细胞瘤 (GBM) 的活性。 | |||
T9033 |
BTYNB
MDK6620,BTYNB IMP1 Inhibitor |
Others; c-Myc; NF-κB | Cell Cycle/Checkpoint; NF-κB; Others |
BTYNB (MDK6620) 是IMP1结合 c-Myc mRNA 的有效选择性抑制剂,IC50为 5 μM。它下调 β-TrCP1 mRNA 并减少NF-κB 的激活。它通过损害 IGF2 mRNA 结合蛋白 1 结合来破坏这种增强子功能,可用于癌症研究。 | |||
T73593 |
PDS-0330
|
Others | Others |
PDS-0330是一种 claudin-1小分子抑制剂抑制。PDS-0330抑制 claudin-1依赖性 CRC 进展,以微摩尔亲和力直接和特异性地与claudin-1结合。PDS-0330通过抑制与转移性癌基因Src 的关联,表现出具有良好药代动力学特性的抗肿瘤和化学增敏活性。PDS-0330干扰claudin-1 / Src 关联以抑制CRC 进展和转移。 | |||
T37807 |
JTV 519 fumarate
|
||
Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo. Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]ryanodine binding to RyR2 irrespective of FKBP12.6 association. Biochem.J. 404 431 PMID:17313373 |Chen et al (2008) Effect of K201, a novel antiarrhythmic drug on calcium handling and arrhythmogenic activity of pulmonary vein cardiomyocytes. Br.J.Pharmacol. 153 915 PMID:17994112 |... | |||
TP2309 |
NEUROTENSIN TFA (39379-15-2 free base)
Pyr-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Tyr-Ile-Leu-OH TFA(55508-42-4 free base),NEUROTENSIN TFA,神经加压素 |
Others | Others |
Neurotensin TFA (39379-15-2 free base) 是一种内源性 13 个氨基酸的神经肽,具有显着的阿片类非依赖性镇痛作用。它在大脑中充当神经递质,在肠道中充当激素,也充当神经调节剂。由于它与多种神经递质系统如多巴胺能、血清素能、谷氨酸能、GABA 能和胆碱能系统。它具有作为人体代谢物、有丝分裂原、神经递质和创伤的作用。 | |||
T9533 |
BC-LI-0186
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide |
Others | Others |
BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) 是选择性抑制亮氨酸 tRNA 合成酶与 Ras 相关的 GTP 结合蛋白 D 相互作用(IC50=46.11 nM)。BC-LI-0186能有效抑制肿瘤相关 MTOR 突变体的特性和雷帕霉素耐药癌细胞的生长,能够用于肺癌的相关研究。 | |||
T23746 |
APA-H-MPO
APAHMPO |
||
APA-H-MPO is a PCAF bromodomain/Tat-AcK50 association inhibitor. | |||
T23745 |
APA-APA-MPO
APA APA MPO,APAAPAMPO |
||
APA-APA-MPO is a PCAF bromodomain/Tat-AcK50 association inhibitor. | |||
T16423 |
p32 Inhibitor M36
M36 |
Others | Others |
p32 inhibitor M36 is an inhibitor of p32 mitochondrial protein. It binds directly to p32 and inhibits the p32 association with LyP-1. | |||
T26382 |
2-Mc-1,4-NHQ
NSC 111552,NSC-111552,NSC111552 |
||
2-Mc-1,4-NHQ, an inhibitor of the Cdc42-PBD interaction, blocks the association of Cdc42 with the PBD. | |||
T33440 |
MK785
MK-785,MK 785 |
||
MK785 is part of the association between inhibition of aortic histamine formation, aortic albumin permeability, and atherosclerosis. Aortic histamine synthesis was inhibited by partial inhibition of aortic histidine decarboxylase (HD) by application of MK | |||
T26342 |
YH16899
YH-16899,YH 16899,BC-K-YH16899 |
||
YH16899 is a KRS-67LR interaction inhibitor by directly blocking the association between KRS and 67LR, suppressing the dynamic movement of the N-terminal extension of KRS and reducing membrane localization of KRS. | |||
T76249L | RNAENFDRF TFA | ||
RNAENFDRF (βIIPKC624-632) TFA 与细胞渗透性肽 TAT47-57 结合,可用于形成抑制性肽 SAMβA。SAMβA 是一种 Mfn1-βIIPKC 结合选择性拮抗剂。SAMβA 是 mitofusin 1-βIIPKC 关联的选择性抑制剂,可改善大鼠心力衰竭。 | |||
TP1777 |
p2Ca
|
||
p2Ca, a naturally processed peptide that derives from a ubiquitous enzyme, alpha-ketoglutarate dehydrogenase, and is recognized in association with the class I MHC protein, Ld, by a CTL clone (2C). | |||
T76249 |
RNAENFDRF
|
||
RNAENFDRF (βIIPKC624-632) 与细胞渗透性肽 TAT47-57 结合,可用于形成抑制性肽 SAMβA。SAMβA 是一种 Mfn1-βIIPKC 结合选择性拮抗剂。SAMβA 是 mitofusin 1-βIIPKC 关联的选择性抑制剂,可改善大鼠心力衰竭。 | |||
T69875 | ProMMP-9 inhibitor-3c | ||
ProMMP-9 inhibitor-3c is a potent and specific proMMP-9 inhibitor which disrupts f MMP-9 homodimerization and prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR. | |||
T80628 |
Myristoyl tetrapeptide-12
|
TGF-beta/Smad | Stem Cells |
Myristoyl tetrapeptide-12 直接激活SMAD2,并促使SMAD3与DNA结合。该化合物能有效促进毛发,特别是睫毛的生长。 | |||
T71000 |
RO-5328673
|
||
RO-5328673 is a dual NK2/NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of g... | |||
T71058 |
Doramapimod HCl
|
||
Doramapimod HCl is the salt form of Doramapimod, a member of the N-pyrazole-N'-naphthly urea class of p38MAPK inhibitors, which binds to the kinase with both slow association and dissociation rates. BIRB -796 has entered clinical trials for the treatment of autoimmune diseases. | |||
T38753 |
CR-1-31-B
|
||
CR-1-31-B, a synthetic rocaglate, acts as a highly potent inhibitor of eIF4A. By disrupting the interaction between eIF4A and RNA, it effectively obstructs the initiation phase of protein synthesis. Specifically, CR-1-31-B interferes with the association between Plasmodium falciparum eIF4A (PfeIF4A) and RNA. Additionally, CR-1-31-B induces apoptosis in neuroblastoma and gallbladder cancer cells [4]. | |||
T81899 | LY836 | iGluR | Membrane transporter/Ion channel; Neuroscience |
LY836是口服活性神经保护剂,有效阻断皮层神经元中PSD95-nNOS的关联,适用于缺血性脑卒中研究。 | |||
T78220 |
SAMβA TFA
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
SAMβA TFA结合了细胞渗透性肽TAT47-57,作为Mfn1-βIIPKC互作的选择性拮抗剂。该化合物是mitofusin 1-βIIPKC相互作用的选择性抑制剂,能够有效改善大鼠心力衰竭状况。 | |||
T73261 |
C5aR-IN-1
|
||
C5aR-IN-1 是一种有效的C5aR 抑制剂。C5a 水平升高与自身免疫性疾病和炎症性疾病等疾病有关。C5aR-IN-1 具有研究炎症性疾病的潜力。 | |||
T61871 | DC-LC3in-D5 | ||
DC-LC3in-D5 is a chemical compound that functions as an autophagy inhibitor by diminishing the process of LC3B lipidation. It forms a binding association with LC3B, disrupting the LC3B-LBP2 interaction with an IC50 of 200 nM. This compound, DC-LC3in-D5, exhibits potential for application in anti-HCV or combination cancer treatments by effectively inhibiting autophagy [1]. | |||
T69401 |
MIND4-17
|
||
MIND4-17为一种NRF2激活剂,通过共价修饰Keap1的C151残基发挥作用。该化合物能破坏Keap1-Nrf2之间的结合,进而促进Nrf2蛋白的稳定性及其向核内的迁移,显示出显著的抗氧化活性。 | |||
T80514 |
TAT-SAMβA
|
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
TAT-SAMβA为RNAENFDRF (SAMβA) 与TAT47-57蛋白衍生肽结合形成的肽类化合物,作为Mfn1-βIIPKC结合的选择性拮抗剂。该化合物能够保护小鼠胚胎成纤维细胞(MEFs)免遭氧化应激诱导的细胞毒性。 | |||
T36798L |
SW2_110A acetate
|
Histone Methyltransferase | Chromatin/Epigenetic |
SW2_110A acetate 是一种选择性的,细胞渗透性的chromobox 同源蛋白CBX8抑制剂(Kd = 800 nM),结合CBX8 N 端色域(ChD)。SW2_110A acetate 对CBX8 N 有很高的亲和力,抑制CBX8与细胞染色质的关联,抑制MLL-AF9诱导的THP1白血病细胞增殖。 | |||
T76306 |
Adipokinetic hormone I (Locusta migratoria)
|
||
Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I) 是昆虫脂肪运动激素(AKH)类,可促进脂肪体内cAMP水平升高。AKH通过与AKH受体结合,并通过刺激性鸟嘌呤核苷酸结合蛋白(Gs)偶联,促进cAMP生成及糖原磷酸化酶活化,从而控制飞蝗动员脂肪体存储的碳水化合物和脂质。 | |||
T76366 |
CART (55-76), rat
|
||
CART (55-76), rat 为一种神经肽,构成CART (55-102)的N端片段,属于鼠源性饱腹感因子,具有显著的抑食作用,并与瘦素及神经肽Y关系紧密。此外,CART (55-76), rat 还能诱发与焦虑和压力相关的行为。 | |||
T82610 |
DA-PROTAC
|
PROTACs | PROTAC |
DA-PROTAC是Atox1和CCS铜离子转运蛋白的有效PROTAC降解剂。该化合物能够与Atox1和CCS结合形成复合体,进而与E3连接酶相结合,引起Atox1和CCS的泛素化水平增加,最终通过蛋白酶体途径导致这两种蛋白的降解。DA-PROTAC在三阴性乳腺癌的研究中有应用潜力。 | |||
T69603 |
BR103354
|
||
BR103354 is a novel fibroblast activation protein (FAP) inhibitor with anti-diabetic and anti-steatotic effects. BR103354 inhibited FAP with an IC50 value of 14 nM, showing high selectivity against dipeptidyl peptidase (DPP)-related enzymes and prolyl oligopeptidase (PREP). BR103354 exhibited good pharmacokinetic properties as evidenced by oral bioavailability of 48.4% and minimal hERG inhibition. Single co-administration of BR103354 with hFGF21 reduced nonfasting blood glucose concentrations, i... | |||
T76365 |
CART (1-39), Human, Rat
|
||
CART (1-39), Human, Rat, 是一种由其1至39个残基构成的神经肽, 具有明显的减少食欲作用, 被认为是鼠类的饱腹因子, 并与瘦素及神经肽Y有着紧密的联系。它能有效抑制正常及饥饿状态下的摄食行为, 同时也能引发焦虑与压力相关的反应。 | |||
T82108 | ICMT-IN-35 | ||
ICMT-IN-35(即compound 10n),作为FTPA-triazole类ICMT抑制剂(IC50=0.8 μM),能被哺乳动物细胞吸收并阻断K-Ras膜定位,进而诱导K-Ras错定位。ICMT-IN-35对ICMT+/+MEF细胞表现出选择性细胞毒性,对转移性胰腺癌细胞系展示低微摩尔级别活性(IC50=0.8 μM)。 | |||
T76059 |
SAH-SOS1A TFA
|
||
SAH-SOS1A TFA 是一种基于肽的SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A TFA 以纳摩尔亲和力 (EC50=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, Q61H) 结合,直接和独立地阻断核苷酸结合。SAH-SOS1A TFA 损害 KRAS 驱动的癌细胞活力,并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。 | |||
T75806 |
Lyn peptide inhibitor TFA
|
||
Lyn peptide inhibitor TFA 是一种有效的,可以细胞渗透的抑制剂,抑制Lyn 偶联的IL-5受体相关信号通路,同时保持其他信号的完整。Lyn peptide inhibitor TFA 可以阻断 Lyn 的激活,抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基结合。Lyn peptide inhibitor TFA 可用于哮喘、过敏等嗜酸性疾病的研究。 | |||
T83506 |
[Asn23]-beta-Amyloid (1-42), iowa mutation
|
||
[Asn23]-beta-Amyloid (1-42), iowa mutation 是具有生物活性的肽,与阿尔茨海默病中的一种严重神经病理状况——大脑淀粉样蛋白血管病 (CAA) 密切相关。这种变异是由于在 APP 694 位点发生了错义突变,其中 Asp 23 被 Asn 取代,导致的。该变异形式的β-淀粉样肽倾向于更快聚集,形成具有毒性的原纤维。 | |||
T36027 |
DEPMPO-biotin
|
||
DEPMPO is a nitrone that is used to spin trap reactive O-, N-, S-, and C-centered radicals and allow their characterization when used in association with electron spin resonance. It is noted for the stability of adducts formed. DEPMPO can be used in vitro or in vivo, as it crosses lipid bilayer membranes and is a good trapping agent in biological systems. DEPMPO-biotin is a biotinylated form of DEPMPO which retains the outstanding persistency of its adducts. The biotin moiety offers an effective... | |||
T83951 |
TM2 TEAD inhibitor
|
||
TM2 TEAD抑制剂是一种有效并且可逆的TEA领域转录因子抑制剂(IC50为TEAD4自动棕榈酰化和TEAD2棕榈酰化分别为38 nM和156 nM)。它抑制TEAD-YAP的结合和转录活性。TM2 TEAD抑制剂在YAP依赖型癌症细胞中,无论是单独使用还是与MEK抑制剂联合使用,都显示出强大的抗增殖效果。同时抑制体外YAP依赖的肝脏类器官生长。 | |||
T36648 | Tucatinib hemiethanolate | ||
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... | |||
T35789 | Palmitic acid-1-13C | ||
Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 |1. Santos, M.J., López-Jurado, M., Llopis, J., et a... | |||
T35791 | Palmitic acid-13C | ||
Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ... | |||
T36717 |
RWJ-56110 dihydrochloride
|
||
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 . RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell ap... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6343 |
Geldanamycin
格尔德霉素,NSC 122750 |
HSP; Influenza Virus; Tyrosine Kinases; Antibacterial; Antibiotic | Cytoskeletal Signaling; Metabolism; Microbiology/Virology; Tyrosine Kinase/Adaptors |
Geldanamycin 是一种 HSP90 抑制剂(Kd:1.2 μM),可特异性破坏糖皮质激素受体 (GR)/HSP 的结合。 | |||
TN1048 |
Cnidilin
Knidilin |
||
Cnidilin (Knidilin) 存在与Angelica dahurica 根中,具有高BBB 通透性,在治疗中枢神经系统疾病方面具有药代动力学潜力。 | |||
T4767 |
Formamide
甲酰胺,Carbamaldehyde,Methanamide,NSC 748,Formimidic acid |
Others; Endogenous Metabolite | Metabolism; Others |
Formamide (NSC-748) 是甲酸的酰胺衍生物,被用作许多离子化合物的溶剂。 | |||
TN2775 |
2-Methoxystypandrone
|
MMP; BCL; IκB/IKK; GSK-3; TNF; NOS; NF-κB; Wnt/beta-catenin; COX; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; NF-κB; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells |
2-Methoxystypandrone displays an immunomodulatory effect in a cellular model, it blocks inflammatory responses by impairing NF-κB signaling to limit the inflammation and oxidative stress for preservation of BBB integrity. 2-Methoxystypandrone concomitant | |||
T36563 |
(E)-Guggulsterone
|
||
Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy... |