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Cat. No. | Product Name | ||
---|---|---|---|
L9300 | 大环化合物库 | 210 compounds | |
210 种活性已知的大环化合物,用于高通量、高内涵筛选; |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8684 |
Sotorasib
AMG-510 |
Ras | GPCR/G Protein; MAPK |
Sotorasib (AMG-510) 是一种 KRAS G12C 共价抑制剂,具有口服活性和选择性。Sotorasib 与 KRAS G12C 非活性构象的 GDP 状态结合,抑制 KRAS 及其下游信号的传导。Sotorasib 对 KRAS G12C 突变肿瘤具有抑制活性。 | |||
T7194 |
CM-272
|
Apoptosis; DNA Methyltransferase; Histone Methyltransferase | Apoptosis; Chromatin/Epigenetic |
CM-272 是一种可逆底物竞争性双重G9a/DNA 甲基转移酶选择性抑制剂,具有抗肿瘤活性。它抑制细胞增殖并促进细胞凋亡,诱导干扰素刺激的基因和免疫原性细胞死亡。它抑制G9a、DNMT1、DNMT3A、DNMT3B 和GLP,IC50分别为 8 nM、382 nM、85 nM、1200 nM 和 2 nM。 | |||
T16813 |
RX-3117
fluorocyclopentenylcytosine,TV-1360 |
Nucleoside Antimetabolite/Analog | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
RX-3117 (fluorocyclopentenylcytosine) 是一种新型的胞苷类似物,在几种癌细胞系中显示出抗癌活性,包括对吉西他滨耐药的变体。 | |||
T8842 |
IMT1B
3-Piperidinecarboxylic acid, 1-[(2R)-2-[[4-(2-chloro-4-fluorophenyl)-2-oxo-2H-1-benzopyran-7-yl]oxy]-1-oxopropyl]-, (3S)-,LDC203974 |
Others; DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Others |
IMT1B (LDC203974) 是一种特异性的、具有口服活性的、非竞争性的线粒体 RNA 聚合酶 (POLRMT) 别构抑制剂,能够抑制线粒体 DNA (mtDNA) 的表达,具有抗肿瘤活性。 | |||
T26866 |
BMS-960
BMS 960,BMS960 |
S1P Receptor | GPCR/G Protein |
BMS-960是一种 S1P 激动剂,具有潜在的抗肿瘤活性,可用于研究癌症。 | |||
T28911 |
Tafetinib
SIM-010603,SIM010603,SIM 010603 |
Tyrosine Kinases | Tyrosine Kinase/Adaptors |
Tafetinib (SIM-010603) 是一种新型有效且可口服的酪氨酸激酶抑制剂,具有抗血管生成和抗肿瘤活性。 | |||
T67699L |
ALK/ROS1 inhibitor 2e HCL
(R)-1-(2-((2-methoxy-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(trifluoromethoxy)benzyl)piperidine-3-carboxamide hydrochloride(2365497-12-5 Free base) |
Apoptosis | Apoptosis |
ALK/ROS1 inhibitor 2e HCL 具有抗凋亡、抗增殖和抗肿瘤活性。 | |||
T14893 |
CC-885
|
Others; Ligand for E3 Ligase | Others; PROTAC |
CC-885 是一种 CRBN 蛋白调节剂,有抗肿瘤的潜能。 | |||
T25384 |
Erbulozole
R-55104,R55104,R 55104 |
Microtubule Associated | Cytoskeletal Signaling |
Erbulozole (R 55104) 是一种有效的合成微管抑制剂,具有抗侵袭、抗肿瘤和放射增敏活性,可诱发 Wernicke 脑病样神经毒性。 | |||
T68152 |
Talmetacin
|
Others | Others |
Talmetacin 具有抗炎镇痛和抗肿瘤活性,可用于研究心血管疾病。 | |||
T77728 |
Tubulin polymerization-IN-55
|
Microtubule Associated | Cytoskeletal Signaling |
Tubulin polymerization-IN-55 是一种高效的 Tubulin Polymerization 抑制剂,具有潜在的抗血管生成和抗肿瘤活性,对 A549、K562、HepG2、MDA-MB-231 和 HFL-1 显示出抗增殖作用。 | |||
T25969 |
Poloxin-2
Poloxin2,Poloxin 2 |
PLK | Cell Cycle/Checkpoint |
Poloxin-2 是一种具有有效性和选择性的 Plk1 PBD 抑制剂,具有抗肿瘤活性,可降低HeLa细胞中Plk1的蛋白水平。 | |||
T7670 |
Mavacoxib
|
COX | Immunology/Inflammation; Neuroscience |
Mavacoxib 是口服长效环氧合酶 2 选择性抑制剂,是长效的非甾体类抗炎药,用于犬退化性关节病相关的炎疼及痛症的研究。 | |||
T83646 |
(S)-OSMI 3
Ent-OSMI-3 |
Others | Others |
(S)-OSMI 3 (Ent-OSMI-3) 具有抗炎抗肿瘤活性,可用以研究糖尿病和神经退行性疾病。 | |||
T61486 |
DHFR-IN-4
|
DHFR | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism |
DHFR-IN-4 是一种高效的二氢叶酸还原酶 (DHFR) 抑制剂,具有抗肿瘤活性,抑制 EGFR 和 HER2 ,可用于研究胰腺癌。 | |||
T64167 |
Ifebemtinib
IN-10018,BI-853520 |
FAK | Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Ifebemtinib (BI-853520) 是一种具有口服活性和强效性的粘附斑激酶 (FAK) 抑制剂 (IC50=1 nM),具有抗肿瘤活性,可抑制恶性胸膜间皮瘤中的球状体形成和原位肿瘤生长,可用于研究乳腺癌和卵巢癌。 | |||
T77407 |
Ensituximab
NPC-1C,NEO-102,NEO-101 |
||
Ensituximab (NEO-102) 是一种准对 MUC5AC 变体的选择性 IgG1 单克隆抗体,具有抗肿瘤活性,抑制结直肠癌和胰腺癌。 | |||
T77733 |
TNKS-2-IN-2
|
Wnt/beta-catenin | Cytoskeletal Signaling; Stem Cells |
TNKS-2-IN-2 是一种新型高效的 TNKS2 选择性抑制剂(IC50: 22 nM),具有潜在的抗肿瘤活性,可用于研究结肠癌肺癌和乳腺癌。 | |||
T35916 |
Simotinib
AL-6802,SIM-6802 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Simotinib (AL-6802) 是一种具有选择性和口服生物活性的 EGFR 酪氨酸激酶抑制剂( IC50 :19.9 nM),具有抗肿瘤活性,可用于研究非小细胞性肺癌。 | |||
T15771 |
Lobaplatin
D-19466,络铂 |
DNA Alkylation | DNA Damage/DNA Repair |
Lobaplatin (D-19466) 是一种铂 (II) 复合物的非对映混合物,是一种有前途的抗肿瘤化疗药物,在多种肿瘤类型的患者中具有活性。 | |||
T36848 |
Combretastatin A-1
Combretastatin A1 |
Akt; Microtubule Associated | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
Combretastatin A-1 是一种有效的微管抑制剂,具有抗肿瘤和抗血管活性,通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路发挥作用,可用于研究肝癌。 | |||
T72029 |
CDK8-IN-13
|
Apoptosis; CDK | Apoptosis; Cell Cycle/Checkpoint |
CDK8-IN-13是一种 CDK8抑制剂(IC50:51.9 nM),具有强效性、选择性和口服活性。CDK8-IN-13能诱导细胞凋亡,降低了 p-STAT1 S727和p-STAT5 S726的表达。CDK8-IN-13表现出抗肿瘤活性。 | |||
T64066 |
CSF1R-IN-3
|
c-Fms; CSF-1R | Tyrosine Kinase/Adaptors |
CSF1R-IN-3是一种口服有效的 CSF-1R 抑制剂,IC50值为2.1nM。CSF1R-IN-3对结直肠癌细胞具有抗增殖活性。CSF1R-IN-3 通过抑制巨噬细胞的迁移,诱导 M2 型巨噬细胞重新编程为 M1 型巨噬细胞,从而表现出抗肿瘤作用和提高免疫力的作用,展现对结直肠癌细胞的活性。 | |||
T33701 |
NM-3
NM-3,isocoumarin,NM 3,Isocoumarin NM-3,NM3 |
Apoptosis; Reactive Oxygen Species | Apoptosis; Immunology/Inflammation; Metabolism; NF-κB |
NM-3 是一种可口服的抗血管生成的抑制剂,具有抗肿瘤活性。NM-3在体外和体内可当作辐射调节剂使用。NM-3抑制血管内皮生长因子(VEGF),从而抑制内皮细胞的增殖。NM-3与活性氧的机制诱导细胞凋亡有关。 | |||
T15615 |
JND3229
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
JND3229 是一种可逆性的 EGFRC797S 抑制剂,对 EGFRL858R/T790M/C797S、EGFRWT 和 EGFRL858R/T790M 的 IC50 值分别为 5.8、6.8 和 30.5 nM。JND3229 具有较好的抗增殖活性,能有效地抑制体内肿瘤的生长。JND3229 可用于癌症,尤其是非小细胞癌的研究。 | |||
T27417L |
Glutathione arsenoxide hydrochloride
GSAO HCl,Glutathione arsenoxide hydrochloride(1271726-51-2 Free base) |
Apoptosis; AChR | Apoptosis; Neuroscience |
Glutathione arsenoxide hydrochloride (Glutathione arsenoxide hydrochloride(1271726-51-2 Free base)) 是一种潜在的抗癌活性分子和肿瘤代谢抑制剂。Glutathione arsenoxide hydrochloride 靶向线粒体内膜腺嘌呤核苷酸转移酶 (ANT),对细胞增殖有抑制作用,促进细胞凋亡。Glutathione arsenoxide hydrochloride 可用于识别如蛋白质二硫异构酶一样的细胞表面蛋白质。 | |||
T30759 |
CB 1837
CB1837,CB-1837,AI3-51871,NSC 3375 |
Others | Others |
CB 1837 is an anti-tumour agent. | |||
T27891 |
LY195448 HCl
LY195448,UNII-BR0DFE3GF6,LY-195448 |
Others | Others |
LY195448 HCl is a phenethanolamine shown anti-tumour activity. It blocks cells at metaphase. | |||
T27873 |
LY 135114
LY135114,LY-135114 |
Others | Others |
LY 135114 is a metabolite of LY 195448, which is a phenethanolamine with anti-tumour activity. | |||
T62601 |
Anticancer agent 48
|
Others | Others |
Anticancer agent 48 (compound 48) 是一种广谱抗癌剂,其表现出抗增殖活性。Anticancer agent 48 对微管蛋白聚合具有抑制作用。Anticancer agent 48 在体内显示抗肿瘤活性。Anticancer agent 48 具有潜力进行实体瘤和血液肿瘤的研究。主语 | |||
T26469 |
A-176120
|
Others | Others |
A-176120 is a potent farnesyl pyrophosphate (FPP) analogues, it selectively inhibits farnesyltransferase. It has anti-angiogenic potential and may reduce H-ras NIH3T3 tumour growth. | |||
T64128 |
Antitumor agent-56
|
Others | Others |
Antitumor agent-56 是一种口服具有活力的 triptolide 衍生物,能够明显抑制黑色素瘤的生长,表现出抗肿瘤、抗炎和 NO 释放作用。 | |||
T62828 |
FRα-IN-1
|
Others | Others |
FRα-IN-1 (Compound 4) 是一种肿瘤靶向剂。FRα-IN-1 对 FRα 和 FRβ 表达细胞表现出选择性的抗癌效果。 | |||
T62602 |
Anticancer agent 49
|
Others | Others |
Anticancer agent 49 (compound 69) 是一种广谱抗癌剂,其表现出抗增殖活性。Anticancer agent 49 对微管蛋白聚合具有抑制作用。Anticancer agent 49 在体内显示抗肿瘤活性。Anticancer agent 49 具有潜力进行实体瘤和血液肿瘤的研究。 | |||
T62875 |
NF-κB-IN-3
|
Others | Others |
NF-κB-IN-3 (Compound 2) 是一种 NF-κB 抑制剂 (IC50: 0.70 μM),能够用作抗肿瘤剂。 | |||
T60590 |
Chloropyramine
|
Others | Others |
Chloropyramine 是竞争性可逆 H1 受体拮抗剂,可用于过敏性疾病的研究,例如结膜炎和支气管哮喘。Chloropyramine 表现出抗乳腺癌活性。 | |||
T63138 |
PRMT5-IN-16
|
Others | Others |
PRMT5-IN-16 (Compound 20) 是一种 PRMT5 抑制剂,具有抗肿瘤作用。其中 PRMT5 是一种蛋白质精氨酸甲基转移酶,是新型的与表观遗传修饰相关的抗肿瘤靶点。 | |||
T62970 |
CDK1-IN-1
|
Others | Others |
CDK1-IN-7 是一种 CDK1 的有效抑制剂,对 CDK1/CycB 的 IC50 值为 161.2 nM。CDK1-IN-7 通过凋亡内在途径以 p53 依赖的方式诱导细胞凋亡。CDK1-IN-7 能够选择性作用于肿瘤组织,并具有潜在的抗增殖作用。CDK1-IN-7 是一种潜在的靶向抗肿瘤药物。 | |||
T64025 |
Top/HDAC-IN-2
|
Others | Others |
Top/HDAC-IN-2 (45b) 是 Top 和 HDAC 的双重抑制剂,能够诱导细胞凋亡,表现出显著的抗肿瘤作用。 | |||
T73186 |
HPK1-IN-31
|
Others | Others |
HPK1-IN-31 是一种具有口服活性的造血祖细胞激酶 1 (HPK1) 抑制剂,IC50值为 0.8 nM。HPK1-IN-31 具有抗肿瘤活性,在免疫治疗方面具有巨大的潜力。 | |||
T72976 |
TGFβRI-IN-6
|
Others | Others |
TGFβRI-IN-6 是一种有效的TGFβRI 抑制剂,IC50值为 0.55 nM。TGFβRI-IN-6 具有增强抗肿瘤免疫力的潜力。 | |||
T63861 |
CCT373566
|
Others | Others |
CCT373566 是一种有效的、具有口服活性的转录抑制因子 BCL6降解剂 (IC50: 2.2 nM)。CCT373566 在体外表现出显著的抗增殖作用,在体内能够减少肿瘤生长。 | |||
T63159 |
Anticancer agent 28
|
Others | Others |
Anticancer agent 28 在体内 H22 同种异体移植小鼠中具有良好的抗肿瘤作用。Anticancer agent 28 对 K562 细胞的作用是 Oridonin 的50倍,其 IC50 值为 0.09 μM。 | |||
T63109 |
Y08284
|
Others | Others |
Y08284 是一种选择性的、高效的、口服具有活力的 CBP bromodomain 抑制剂 (IC50: 4.21 nM)。Y08284 能够抑制前列腺癌细胞系 LNCaP、C4-2B 和 22Rv1 的增殖,并具有抗肿瘤效果。 | |||
T64296 |
TIY-7
|
Others | Others |
TIY-7 是一种选择性、口服具有活力的原肌球蛋白受体激酶 (TRK) 抑制剂。TIY-7 能够抑制 TRKA 酶 (IC50: 2.9 nM)、TRKAG595R 酶 (IC50: 1.1 nM)、TRKAG667C 酶 (IC50: 0.7 nM)、TRKAF589L 酶 (IC50: 0.8 nM)、TRKCG623R 酶 (IC50: 0.8 nM)、TRKCG696A 酶 (IC50: 0.2 nM)。TIY-7 在小鼠异种移植模型中表现出抗肿瘤效果。 | |||
T64093 |
KRAS G12C inhibitor 44
|
Others | Others |
KRAS G12C inhibitor 44 是一种有效的、口服具有活力的 KRAS G12C 抑制剂。KRAS G12C inhibitor 44 在 MIA PaCA-2 (IC50: 0.016 μM)、H358 细胞 (IC50: 0.028 μM) 中表现出抗增殖作用。KRAS G12C inhibitor 44 在体内具有抗肿瘤活性。 | |||
T62598 |
Pitavastatin sodium
|
Others | Others |
Pitavastatin (NK-104) sodium 是一种有效的羟甲基戊二酰-CoA(HMG-CoA) 还原酶抑制剂,也是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。Pitavastatin sodium 在 HepG2 细胞中,能够抑制乙酸合成胆固醇 (IC50: 5.8 nM) 。Pitavastatin sodium 表现出抗动脉粥样硬化、抗哮喘、抗骨关节炎、神经保护、抗肿瘤、肝保护和肾保护作用。 | |||
T63922 |
ERα degrader 5
|
Others | Others |
ERα degrader 5 是一种口服具有活力的、选择性的雌激素受体 (estrogen receptor (ER)) 降解剂,能够作用于 ERα (EC50: 1.1 nM)。ERα degrader 5 在体内显示抗肿瘤效果。 | |||
T62763 |
VEGFR-2-IN-12
|
Others | Others |
VEGFR-2-IN-12 (compound 6g) 是一种 2-oxoquinoxalinyl-1,2,4-triazole,是一种 VEGFR-2 的有效抑制剂 (IC50: 0.037 μM)。VEGFR-2-IN-12 能够高度抑制 MCF-7 细胞的生长 (GI50: 1.6 μM)。VEGFR-2-IN-12 具有抗肿瘤作用。 | |||
T63934 |
PAK4-IN-1
|
Others | Others |
PAK4-IN-1 是一个选择性的、有效的、口服具有活力的 PAK4 抑制剂,在酸性和中性条件下都很稳定。PAK4-IN-1 在体内表现出良好的抗肿瘤作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4601 |
9-Methoxycanthin-6-one
|
Others | Others |
9-Methoxycanthin-6-one 是存在于完整植株和不同外植体的愈伤组织中的 Canthin-6-one 生物碱,具有抗肿瘤作用。 | |||
TN1582 |
Compound TN1582(SC)
|
Antiviral | Immunology/Inflammation |
Dihydromollugin 是在 Rubia cordifolia 中发现的萘甲酸酯,可能具有抗肿瘤、抑制病毒和其他活性。 | |||
T2798 |
Esculetin
秦皮乙素,二羟基香豆素,Aesculetin,Cichorigenin |
Lipoxygenase; Akt; PI3K | Cytoskeletal Signaling; Metabolism; PI3K/Akt/mTOR signaling |
Esculetin (Cichorigenin) 是主要提取自水曲柳的树皮中的活性成分。它能够抑制PI3K/Akt 途径,阻碍血小板衍生生长因子诱导的气道平滑肌细胞表型转换。它具有抗氧化,抗炎和抗肿瘤的活性。 | |||
T7468 |
(-)-α-Terpineol
alpha-松油醇,(-)-α-松油醇,α-Terpineol |
Others | Others |
(-)-α-Terpineol 是白葡萄酒中重要的香气化合物,是一种单萜化合物。 | |||
TN3917 |
Echitamine
|
Others | Others |
Echitamine chloride possesses anti-tumour activity in-vitro and in-vivo. | |||
T4366 |
Quinovic acid
|
NF-κB; Caspase | Apoptosis; NF-κB; Proteases/Proteasome |
Quinovic acid shows some anti-tumour activities, quinovic acid glycosides have a potent inhibitory effect on the growth of human bladder cancer cell lines by inducing apoptosis through modulation of NF-κB. |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-00491 |
IL-18BP Protein, Cynomolgus, Recombinant (His)
Igifbp,Interleukin-18-binding protein,IL-18BP |
Cynomolgus | HEK293 Cells |
Cytokines were the first modern immunotherapies to produce durable responses in patients with advanced cancer,components of the interleukin-18 (IL-18) pathway are upregulated on tumour-infiltrating lymphocytes, suggesting that IL-18 therapy could enhance anti-tumour immunity. IL-18BP, a high-affinity IL-18 decoy receptor, is frequently upregulated in diverse human and mouse tumours and limits the anti-tumour activity of IL-18 in mice. IL-18BP Protein, Cynomolgus, Recombinant (His) is expressed i... | |||
TMPK-00492 |
IL-18BP Protein (Primary Amine Labeling), Cynomolgus, Recombinant (His), Biotinylated
Igifbp,Interleukin-18-binding protein,IL-18BP |
Cynomolgus | HEK293 Cells |
Cytokines were the first modern immunotherapies to produce durable responses in patients with advanced cancer,components of the interleukin-18 (IL-18) pathway are upregulated on tumour-infiltrating lymphocytes, suggesting that IL-18 therapy could enhance anti-tumour immunity. IL-18BP, a high-affinity IL-18 decoy receptor, is frequently upregulated in diverse human and mouse tumours and limits the anti-tumour activity of IL-18 in mice. IL-18BP Protein (Primary Amine Labeling), Cynomolgus, Recombi... | |||
TMPK-00082 |
IL-18BP Protein, Human, Recombinant (His & Avi), Biotinylated
Igifbp,IL-18BP,IL-18BPA |
Human | HEK293 Cells |
Cytokines were the first modern immunotherapies to produce durable responses in patients with advanced cancer,components of the interleukin-18 (IL-18) pathway are upregulated on tumour-infiltrating lymphocytes, suggesting that IL-18 therapy could enhance anti-tumour immunity. IL-18BP, a high-affinity IL-18 decoy receptor, is frequently upregulated in diverse human and mouse tumours and limits the anti-tumour activity of IL-18 in mice. IL-18BP Protein, Human, Recombinant (His & Avi), Biotinylated... | |||
TMPK-00456 |
IGF1R/CD221 Protein, Human, Recombinant (aa 31-932, His & Avi), Biotinylated
CD221,MGC142172,IGFIR,IGFR,MGC18216,JTK13,IGF-I R,IGF-1R,IGF... |
Human | HEK293 Cells |
The type 1 IGF receptor (IGF1R) is a transmembrane tyrosine kinase that is frequently overexpressed by tumours, and mediates proliferation and apoptosis protection. IGF signalling also influences hypoxia signalling, protease secretion, tumour cell motility and adhesion, and thus can affect the propensity for invasion and metastasis. Therefore, the IGF1R is now an attractive anti-cancer treatment target. IGF1R/CD221 Protein, Human, Recombinant (aa 31-932, His & Avi), Biotinylated is expressed in ... | |||
TMPK-00658 |
IGF1R/CD221 Protein, Cynomolgus, Recombinant (His)
CD221,IGFR,IGF1R,MGC142172,MGC18216,IGF-1R,IGF-I receptor,MG... |
Cynomolgus | HEK293 Cells |
The type 1 IGF receptor (IGF1R) is a transmembrane tyrosine kinase that is frequently overexpressed by tumours, and mediates proliferation and apoptosis protection. IGF signalling also influences hypoxia signalling, protease secretion, tumour cell motility and adhesion, and thus can affect the propensity for invasion and metastasis. Therefore, the IGF1R is now an attractive anti-cancer treatment target. IGF1R/CD221 Protein, Cynomolgus, Recombinant (His) is expressed in HEK293 mammalian cells wit... | |||
TMPK-00455 |
IGF1R/CD221 Protein, Human, Recombinant (His & Avi)
MGC142172,IGF-I receptor,IGF-I R,IGF-1R,MGC18216,MGC142170,I... |
Human | HEK293 Cells |
The type 1 IGF receptor (IGF1R) is a transmembrane tyrosine kinase that is frequently overexpressed by tumours, and mediates proliferation and apoptosis protection. IGF signalling also influences hypoxia signalling, protease secretion, tumour cell motility and adhesion, and thus can affect the propensity for invasion and metastasis. Therefore, the IGF1R is now an attractive anti-cancer treatment target. IGF1R/CD221 Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells wi... |