52
7
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T11526 |
DPP-IV-IN-2
H-Lys(4-nitro-Z)-pyrrolidide |
DPP-4 | Proteases/Proteasome |
DPP-IV-IN-2 (H-Lys(4-nitro-Z)-pyrrolidide) 是二肽基肽酶 IV 和DP8/9的抑制剂, IC50分别为 0.1 和 0.95 μM。 | |||
T7743 |
ANGIOTENSIN IV TFA(12676-15-2(free base))
|
RAAS | Endocrinology/Hormones |
ANGIOTENSIN IV TFA(12676-15-2(free base)) 是一种不太有效的血管紧张素 AT1 受体激动剂。 | |||
T2283 |
PX-12
2-[(1-甲基丙基)二硫代]-1H-咪唑,IV-2,PX12 |
Thioredoxin | Metabolism |
PX-12 (PX12) 是一种可逆的硫氧还蛋白-1(Trx-1)抑制剂,能够抑制 MCF-7 细胞(IC50:1.9 μM)和HT-29 细胞(IC50:2.9 μM)的生长。 | |||
T4019 |
Cambinol
SIRT1/2 Inhibitor IV,NSC 112546 |
Apoptosis; Phospholipase; Sirtuin | Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism |
Cambinol (SIRT1/2 Inhibitor IV) 是一种SIRT1和SIRT2的抑制剂,IC50值分别为 56 μM 和 59 μM。它是中性鞘磷脂酶的外泌体抑制剂。 | |||
T23357 |
SIRT1/2 Inhibitor IV
|
Others | Others |
SIRT1/2 Inhibitor IV (cannabinol) is a small-molecule inhibitor of SIRT1 and SIRT2 with IC50 values of 56 μM and 59 μM, respectively. | |||
T36524 |
IKK2-IN-4
5-Phenyl-2-ureidothiophene-3-carboxylic Acid Amide,IKK2 Inhibitor IV |
IκB/IKK; TNF | Apoptosis; NF-κB |
IKK2-IN-4 (IKK2 Inhibitor IV)是一种高效的 IKK-2 抑制剂,IC50 值为 25 nM。IKK2-IN-4 对 LPS 诱导的 PBMC 中 TNFα 的产生有抑制作用。 | |||
T22276 |
Bis(maltolato)oxovanadium(IV)
双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV) |
Phosphatase; Others | Metabolism; Others |
Bis(maltolato)oxovanadium(IV) (BMOV) 是一种有效的胰岛素增敏剂,也是一种有效的、竞争性的、可逆的、口服具有活性的光谱蛋白酪氨酸磷酸酶 (PTP) 抑制剂。它抑制HCPTPA,PTP1B,HPTPβ和SHP2的IC50分别为 126 nM,109 nM,26 nM 和 201 nM。 | |||
T60087 |
cFMS Receptor Inhibitor IV
5-cyano-N-(2,5-di(piperidin-1-yl)phenyl)furan-2-carboxamide |
c-Fms | Tyrosine Kinase/Adaptors |
cFMS Receptor Inhibitor IV 是 c-Fms 酪氨酸激酶的抑制剂。 | |||
T22337 |
Ganciclovir sodium
RS-21592 sodium,Cytovene IV sodium,2'-Nor-2'-deoxyguanosine sodium,BW 759 sodium,更昔洛韦钠 |
Nucleoside Antimetabolite/Analog; Others; Antifection; HSV | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Microbiology/Virology; Others |
Ganciclovir sodium (Cytovene IV sodium) 是核苷类似物和口服抗病毒药物,具有抗病毒活性,尤其是针对巨细胞病毒和单纯疱疹病毒 1 型。 | |||
T4263 |
BAY 61-3606
2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺,Syk inhibitor IV |
Apoptosis; Syk | Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors |
BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的,ATP 竞争性的可逆选择性Syk 抑制剂。它作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化,也降低 K-rn 细胞裂解物中 Syk 磷酸化。 | |||
T15159 |
Dorzagliatin
HMS5552 |
Glucokinase | Metabolism |
Dorzagliatin (HMS5552) 是双重作用的葡萄糖激酶 (glucokinase;GK) 激活剂,可改善 2 型糖尿病的血糖控制,提高胰腺 β 细胞功能。 | |||
T24546 |
Nrf2-Activator-12G
Nrf2 Activator IV,Nrf2 Activator-IV |
||
Nrf2-Activator-12G is a potent Nrf-2 activator. | |||
T72154 | Topoisomerase IV inhibitor 2 | Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseIV inhibitor 2 (compound 5d) 是一种 DNA 拓扑异构酶 IV 抑制剂,其对 TOPO IV 和 DNA 促旋酶的 IC50 值分别为 0.35 μM 和 0.55 μM。此化合物显示出针对 Staphylococcus aureus Newman 菌株和 Escherichia coli ATCC8739 的抗菌活性,对应的 MIC 值分别为 1.985 μM 和 0.744 μM。 | |||
T72547 | Plm IV inhibitor-2 | ||
Plm IV inhibitor-2 是一种有效的Plm IV 抑制剂,对Plm IV、II 和 I 的IC50分别为24 nM、70 nM 和 0.3 μM。适用于研究Plasmodium 寄生虫引起的疟疾。 | |||
T1502 |
Vildagliptin
维达列汀,NVP-LAF 237,维格列汀,LAF237 |
Apoptosis; Ferroptosis; Proteasome; DPP-4 | Apoptosis; Proteases/Proteasome; Ubiquitination |
Vildagliptin (LAF237) 是一种选择性二肽基肽酶IV (DPP-IV) 抑制剂,在人 Caco-2 细胞中抑制 DPP-IV 的IC50为 3.5 nM。它具有出色的口服生物利用度和降血糖活性。 | |||
T0242L |
Sitagliptin phosphate monohydrate
MK-0431,MK-0431 phosphate monohydrate,西他列汀磷酸盐一水合物 |
Proteasome; DPP-4; Autophagy | Autophagy; Proteases/Proteasome; Ubiquitination |
Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP-IV 抑制剂,在 Caco-2 细胞提取物中的 IC50 为 19 nM。 | |||
T22137 |
PTP Inhibitor IV
|
Others | Others |
PTP Inhibitor IV 是一种有效的蛋白酪氨酸磷酸酶 (PTP) 抑制剂,可选择性抑制 DUSP14 磷酸酶活性(IC50 : 5.21 μM)。PTP Inhibitor IV 对 SHP-2、PTP1B、PTP-ε、PTP Meg-2、PTP-σ、PTP-β 和 PTP-μ具有抑制作用,IC50 分别为 1.8 μM、2.5 μM、8.4 μM、13 μM、20 μM、6.4 μM,和 6.7 μM。PTP Inhibitor IV 通过抑制PTP 活性,影响细胞信号传导,并可能调节与PTP 介导的信号传导事件相关的特定途径。 | |||
T68053 |
Denagliptin
GW823093 |
DPP-4 | Proteases/Proteasome |
Denagliptin是一种小分子二肽基肽酶IV(DPP-4)抑制剂,可用于治疗内分泌于代谢疾病,可用于研究2型糖尿病。 | |||
T21512 |
MMP-2/MMP-9 Inhibitor I
|
MMP | Proteases/Proteasome |
MMP-2/MMP-9-IN-1 是一种有效的、具有高选择性和可口服的 IV 型胶原酶 (MMP-9和MMP-2) 抑制剂,对 MMP-9 和 MMP-2具有抑制作用, IC50分别为 0.24 和 0.3 1μM。MMP-2/MMP-9-IN-1 在肿瘤生长和转移的动物模型中展现出口服活性,可用于研究癌症。 | |||
T21979 |
P32/98 (hemifumarate)
|
||
P32/98 hemifumarate 为二肽基肽酶 IV (DPP4) 抑制剂,可在Zucker糖尿病大鼠模型中改善葡萄糖耐量、提高胰岛素敏感性及增强β细胞反应性,具有预防2型糖尿病的潜力。 | |||
TP1501L |
CTTHWGFTLC, CYCLIC acetate(244082-19-7 free base)
|
MMP | Proteases/Proteasome |
CTTHWGFTLC, CYCLIC acetate(244082-19-7 free base) 是基质金属蛋白酶 (MMP)-2 和 MMP-9 的抑制剂。它也被称为IV 型胶原酶或明胶酶。明胶酶是癌症治疗干预的潜在靶点,这些酶的抑制剂可以防止肿瘤进展。 | |||
T16321 |
NI-42
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
NI-42 是一种用于 BRPF 的结构正交化学探针,是有偏向性的BRPFs 溴结构域 (BRD)抑制剂,BRPF1、2和3的IC50为7.9、48和260 nM; BRPF1、2和3的Kd 值为40、210和940 nM,与非分类 IV BRD 蛋白相比具有很好的选择性。 | |||
T6289 |
Dovitinib
TKI258,多韦替尼,CHIR-258,度维替尼 |
VEGFR; FGFR; FLT; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib (CHIR-258) 是一种口服有效的、多靶点的酪氨酸激酶 (RTK) 抑制剂,具有抗肿瘤作用。 | |||
T6479 |
Dovitinib lactate hydrate
Dovitinib (TKI258) Lactate,多韦替尼,Dovitinib Lactate,TKI258 |
VEGFR; FGFR; FLT; PDGFR; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib lactate hydrate (TKI258) 是一种多靶点的酪氨酸激酶抑制剂,抑制 FLT3,c-Kit,FGFR1/3,VEGFR1/2/3和 PDGFRα/β的 IC50值分别为 1,2,8/9,10/13/8,27/210 nM。 | |||
T1674 |
Nateglinide
那格列奈,A4166,Senaglinide |
Potassium Channel; Proteasome; PPAR | DNA Damage/DNA Repair; Membrane transporter/Ion channel; Metabolism; Proteases/Proteasome; Ubiquitination |
Nateglinide (Senaglinide) 是 D-苯丙氨酸的一种衍生物,是口服有效的、短效促胰岛素释放化合物,也是 DPP IV 抑制剂。 Nateglinide 抑制胰岛 β 细胞中 ATP 敏感的 K+通道。Nateglinide 在 2 型糖尿病中具有研究价值。 | |||
T63964 |
DPP-4/GPR119 modulator 2
|
||
DPP-4/GPR119 modulator 2 是二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50: 0.22 μM),也是一种 GPR119 激动剂 (EC50: 0.95 μM)。DPP-4/GPR119 modulator 2 能够用于研究糖尿病。 | |||
T26941 |
Camegliptin
RO-4876904-001,R1579,RG1579,RO-4876904,R-1579,RG-1579 |
||
Cameglipti, a dipeptidyl peptidase IV (DPP-4) inhibitor, is used potentially for the treatment of type 2 diabetes. | |||
T61076 |
Vildagliptin dihydrate
|
||
Vildagliptin dihydrate (LAF237 dihydrate) is a powerful and stable dipeptidyl peptidase IV (DPP-IV) inhibitor, demonstrating selectivity with an IC50 of 3.5 nM in human Caco-2 cells. This compound exhibits exceptional oral bioavailability and significant antihyperglycemic activity [1]. | |||
T76030 |
Bim BH3, Peptide IV TFA
|
||
BimBH3, Peptide IV TFA 是一种来自 BH3-only proteinBim 的 26 个残基肽,属于Bcl-2蛋白家族的促凋亡家族。 | |||
T72153 |
Topoisomerase IV inhibitor 1
|
Topoisomerase | DNA Damage/DNA Repair |
TopoisomeraseIV inhibitor 2 (compound 7d) 作为DNA拓扑异构酶IV(TOPO IV)抑制剂,展现出高效的活性,其对TOPO IV的IC50值为0.23 μM,而对DNA促旋酶的IC50为0.43 μM。此外,该化合物在抗菌领域同样表现出较强的能力,对金黄色葡萄球菌Nerman菌株(Staphylococcus aureus Newman)和大肠杆菌ATCC8739的最小抑菌浓度(MIC)分别为0.972 μM和0.608 μM。 | |||
T13434 |
β-Secretase Inhibitor IV
|
Others | Others |
β-Secretase Inhibitor IV is a potent, cell-active inhibitor of BACE-1(IC50s of 15.6 and 16.3nM under BACE-1 concentrations of 2 nM and 100 pM, respectively). | |||
T6193 |
Dovitinib Dilactic Acid
Dovitinib (TKI-258) Dilactic Acid,TKI258 Dilactic acid |
VEGFR; FGFR; FLT; c-Kit | Angiogenesis; Tyrosine Kinase/Adaptors |
Dovitinib Dilactic Acid (Dovitinib(TKI-258) Dilactic Acid) 是 Dovitinib 的双乳酸,是一种多靶点 RTK 抑制剂,主要用于 III 类 (FLT3/c-Kit),IC50 为 1 nM/2 nM,对 IV 类 (FGFR1/ 3) 和 V 类 (VEGFR1-4) RTK,IC50 为 8-13 nM,对 InsR、EGFR、c-Met、EphA2、Tie2、IGFR1 和 HER2 的效力较低。 | |||
T68652 | Carmegliptin dihydrochloride | ||
Carmegliptin dihydrochloride is the salt form of Camegliptin (free base), also known as RG-1579 and RO4876904, a dipeptidyl peptidase IV (DPP-4) inhibitor potentially for the treatment of type 2 diabetes. | |||
TP1718 |
Bim BH3, Peptide IV TFA (721885-31-0 free base)
Bim BH3, Peptide IV TFA |
||
Bim BH3, Peptide IV TFA is a 26-site residue of BH3 protein Bim, belonging to the pro-apoptotic group of bcl-2 protein family. | |||
T30169 |
ASP-8497
UNII-GC7THT248G,ASP8497,ASP 8497 |
||
ASP8497 is a potent, long-acting DPP-IV inhibitor that improves glucose tolerance by elevating GLP-1 levels in a glucose-dependent insulin-stimulating manner. The compound is used as a therapeutic agent for impaired glucose tolerance and type 2 diabetes. | |||
T78335 |
Inetetamab
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Inetetamab是一种针对HER2受体结构域IV的单克隆抗体,无论是单药使用还是联合酪氨酸激酶抑制剂,均展现出抗肿瘤活性。 | |||
T81025 |
Teduglutide TFA
ALX-0600 TFA |
||
Teduglutide TFA 是一种具有耐受二肽基肽酶 IV 的胰高血糖素样肽 2 (GLP-2) 类似物,与肠道黏膜营养作用相关。它可用于研究短肠综合征 (SBS) 和克罗恩病 (CD)。 | |||
T73875 |
Fotagliptin benzoate
|
||
Fotagliptin benzoate,作为一种二肽基肽酶IV (DPP-4) 抑制剂(IC50=2.27 nM),在大鼠和狗中展现了安全性,适用于2型糖尿病的研究。 | |||
T73299 |
APE1-IN-2
|
Apoptosis | Apoptosis |
APE1-IN-2(compound AP1)是一种具有抗癌活性的Pt(IV)前体,靶向BER关键蛋白APE1。该化合物能诱导细胞内铂的积累,并激活DNA损伤反应及凋亡信号。 | |||
T70932 | L6H9 | ||
L6H9 is a novel inhibitor of myeloid differentiation factor 2 (MD2), suppressing HG-induced expression of ACE and AT1 receptor and Angiotensin II (AngII) production in renal NRK‐52E cells, resulting in the decrease in fibrosis markers such as TGF-β and collagen IV. | |||
T61481 | TP0480066 | ||
TP0480066, a selective topoisomerase II inhibitor, demonstrates excellent inhibitory activity against DNA gyrase (IC50 = 1.10 nM) and topo IV (IC50 = 62.89 nM). This compound exhibits potent efficacy against multiple bacterial species, including drug-resistant strains. Moreover, TP0480066 displays significant inhibitory activity against N. gonorrhoeae, making it suitable for research on gonorrhea [1] [2]. | |||
TP1501 |
CTTHWGFTLC, CYCLIC
|
||
This cyclic CTT Gelatinase Inhibitor peptide is an inhibitor for matrix metalloproteinases (MMP)-2 and MMP-9. It is also called type IV collagenase or gelatinase. Gelatinases are potential targets of therapeutic intervention in cancer, and inhibitors of t | |||
T75856 |
Huwentoxin-IV TFA
|
||
Huwentoxin-IV TFA是一种具有高效性和选择性的钠通道阻滞剂,能够抑制Nav1.7、Nav1.2、Nav1.3和Nav1.4神经元,其IC50分别为26、150、338和400nM。通过优先结合于神经毒素受体位点4,Huwentoxin-IV TFA特异性地阻断周围神经的Nav1.7亚型。该化合物适用于炎症性及神经性疼痛动物模型的研究。 | |||
T29062 |
UNC3133
UNC 3133,UNC-3133 |
||
UNC3133 is a potent and selective Mer tyrosine kinase (MerTK) inhibitor with IC50 Mer 3.0 nM; Axl 17nM; Tyro 3.31 nM; FLT3 6.6 nM; PO Cmax = 0.023; IV T1/2 = 1.59 h, %F = 16. Mer tyrosine kinase (MerTK) is aberrantly elevated in various tumor cells and ha | |||
T37861 | Talabostat | ||
Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,... | |||
T61054 | Type II topoisomerase inhibitor 1 | ||
Type II topoisomerase inhibitor 1 可用于抗菌领域。Type II topoisomerase inhibitor 1 是大肠杆菌DNA 旋转酶的选择性抑制剂,IC50值为 1.7 nM,并能与 Asp73 残基形成氢键。Type II topoisomerase inhibitor 1 抑制拓扑异构酶 IV 的活性,IC50值为 0.98 μM。 | |||
T76905 | Anbenitamab | ||
Anbenitamab (KN-026) 是一种双特异性抗体,同时靶向人 HER2的胞外结构域 II 和 IV。Anbenitamab 阻断配体依赖性和配体非依赖性 HER2 信号通路。Anbenitamab 的 IgG1Fc 片段结合 FcRγIIIa 介导有效的抗体依赖性细胞介导的细胞毒性 (ADCC) 并抑制肿瘤细胞增殖。Anbenitamab 具有用于 HER2 阳性转移性乳腺癌 (MBC) 研究的潜力。 | |||
T21705 |
8-CPT-Cyclic AMP (sodium salt)
|
||
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium 是环 AMP 依赖性蛋白激酶的选择性激活剂。 8-CPT-Cyclic AMP sodium 也是有效的环 GMP 特异性磷酸二酯酶(PDE VA)抑制剂,IC50为 0.9 μM。 8-CPT-Cyclic AMP sodium 还抑制 PDE III 和 PDE IV,IC50分别为 24 和 25 μM。8-CPT-Cyclic AMP sodium 对 Epac 具有非常高的亲和力,是一种有效的Epac 活化剂。 | |||
T19706 |
Ro 20-1724
Ro-20-1724,4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone,Ro20-1724 |
PDE | Metabolism |
Ro 20-1724 (4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone) 是 cAMP 特异性磷酸二酯酶抑制剂 b>(PDE4/PDE IV),其 Ki=1930 nM,具有神经保护作用。 | |||
T35760 |
Carnaubadiol
|
||
Carnaubadiol is a triterpene that has been found in E. corollata and has antiprotozoal activities.1,2 It is active against L. infantum promastigotes and amastigotes, as well as T. cruzi trypomastigotes (IC50s = 46.2, 7.8, and 14.9 μM, respectively).2 |1. Piatak, D.M., and Reimann, K.A. Plant investigations IV. Corollatadiol A new triterpene from euphorbia corollata. Tetrahedron Lett. 13(44), 4525-4528 (1972).|2. de Almeida, B.C., Araújo, B.Q., Carvalho, A.A., et al. Antiprotozoal activity of ext... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1418 |
Azaleatin
杜鹃黄素,2-(3,4-二羟基苯基)-3,7-二羟基-5-甲氧基苯并吡喃-4-酮 |
DPP-4 | Proteases/Proteasome |
Azaleatin 是分离自Rhododendron 种中的 O-甲基化黄酮醇。它是二肽基肽酶-IV 的抑制剂。它在 2 型糖尿病和肥胖症中有研究的价值。 | |||
T2973 |
Astragaloside IV
AST-IV,黄芪甲苷IV,AS-IV,黄芪皂苷 IV |
MMP; ERK; Estrogen/progestogen Receptor; JNK | Endocrinology/Hormones; MAPK; Proteases/Proteasome |
Astragaloside IV (AS-IV) 是从黄芪中分离得到的一种皂苷,抑制ERK1/2和JNK 激活,在乳腺癌细胞 MDA-MB-231 中,下调(MMP)-2和(MMP)-9的信号通路。 | |||
T3918 |
Ginsenoside Rb3
人参皂苷 Rb3,Gypenoside IV,人参皂苷Rb3 |
NF-κB; COX; NO Synthase | Immunology/Inflammation; Neuroscience; NF-κB |
Ginsenoside Rb3 (Gypenoside IV) 是从三七中提取的一种天然产物。它在 293T 细胞系中抑制 TNFα 诱导的NF-κB 转录活性,IC50为 8.2 μM。它还抑制COX-2和iNOSmRNA 的诱导。 | |||
T2S2215 |
Crebanine
|
Apoptosis; Others; Akt | Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling |
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。 | |||
TN1458 |
Buddlejasaponin IV
|
PARP; Akt; Chk | Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Buddlejasaponin IV has analgesic and anti-inflammatory effects, the inhibitions of the expressions of iNOS, COX-2, TNF-alpha, IL-1beta and IL-6 by blocking NF-kappaB activation. | |||
TN6241 |
Momordicin IV
|
||
Momordicin IV 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN6241,CAS号为 894412-35-2。 | |||
TN3478 | Bacopaside IV | Others | Others |
Bacopaside IV 是一种天然产物,可用于生命科学领域的相关研究。其产品编号为 TN3478,CAS号为 155545-03-2。 |