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Cat. No. | Product Name | Target | Signaling Pathways |
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T40121 |
SHP2-D26
SHP2-D26 |
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SHP2-D26 is a highly potent and effective SHP2 degrader. Its mechanism of action involves the induction of SHP2 degradation through binding to VHL-1 and SHP2 proteins. Additionally, the degradation of SHP2 induced by SHP2-D26 is dependent on neddylation and proteasome activity. | |||
T39640 |
JAB-3068
SHP2-IN-6 |
Phosphatase | Metabolism |
JAB-3068 (SHP2-IN-6) 是一种高效的 SHP2 抑制剂, 具有抗癌抗肿瘤活性,可用于研究乳腺癌肺癌和食道癌。 | |||
T40250 |
SHP2 protein degrader-1
SHP2 protein degrader-1 |
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SHP2 protein degrader-1 is a highly efficient allosteric inhibitor targeting SHP2. It effectively induces degradation of SHP2 protein, resulting in cell apoptosis. This compound shows promising potential for studying diseases associated with SHP2. | |||
T39658 |
RMC-4630
SHP2-IN-7,RMC-4630 |
Phosphatase | Metabolism |
RMC-4630 (SHP2-IN-7) 是 SHP2 的抑制剂。 | |||
T39641 |
SHP2-IN-6 hydrochloride
SHP2-IN-6 hydrochloride |
||
SHP2-IN-6 hydrochloride is a highly potent inhibitor of SHP2 with an IC50 of 25.8 nM. | |||
T12903 |
SHP2 IN-1
|
Others | Others |
SHP2 IN-1 is an allergic SHP2 (PTPN11) inhibitor(IC50 : 3 nM). | |||
T63993 | SHP2 inhibitor LY6 | ||
SHP2 inhibitor LY6 (LY6) 是一种有效的、选择性的 SHP2 抑制剂 (IC50: 9.8 μM)。SHP2 inhibitor LY6 能够阻碍 SHP2 介导的细胞信号传导和增殖。 | |||
T81162 |
SHP2-IN-20
|
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SHP2-IN-20 (compound 193)为SHP2抑制剂,具有3 nM的IC50值,适用于胶质母细胞瘤研究。 | |||
T79108 | SHP2-IN-14 | ||
SHP2-IN-14 (compound 27) 为一种口服生效SHP2变构抑制剂(IC50=7 nM),展示抗肿瘤作用。该化合物能够有效抑止小鼠NCI-H358肿瘤模型生长,且具备优良药代动力学属性和安全性。 | |||
T74430 |
SHP2 protein degrader-2
|
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SHP2protein degrader-2 (SHP2-D26) 是一种SHP2蛋白PROTAC 降解剂。SHP2protein degrader-2 可降低各种癌细胞中SHP2的表达水平。 | |||
T61891 | SHP2-IN-8 | ||
SHP2-IN-8 是一种可逆、非竞争性、选择性、高效性的变构SHP2抑制剂(IC50= 23 nM,Ki= 22 nM),在细胞中也有效果。SHP2-IN-8 能引起显著的热位移(ΔTm = 7.01 ℃)。SHP2-IN-8 可抑制AKT 的磷酸化,诱导 Hela 细胞凋亡 (apoptosis)。 | |||
T79412 |
SHP2-IN-16
|
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SHP2-IN-16(化合物222)作为SHP2抑制剂,具有1 nM的IC50值,适用于胶质母细胞瘤研究。 | |||
T78896 |
SHP2-IN-22
|
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SHP2-IN-22 作为变构抑制剂,靶向SHP2,具有 17.7 nM 的 IC50。该化合物能够有效抑制MIA PaCa-2胰腺癌细胞的增殖、迁移和侵袭行为。SHP2-IN-22 主要用于研究含Kirsten大鼠肉瘤病毒癌基因(KRAS)突变型的癌症。 | |||
T72839 |
SHP2/HDAC-IN-1
|
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SHP2/HDAC-IN-1 是一种变构的 SHP2/HDAC 双重抑制剂,IC50值分别为 20.4 nM (SHP2) 和 25.3 nM ( HDAC1)。SHP2/HDAC-IN-1 通过激活 T 细胞、增强抗原呈递功能和促进细胞因子分泌来触发抗肿瘤免疫反应。SHP2/HDAC-IN-1 可用于癌症的免疫治疗研究。 | |||
T81163 |
SHP2-IN-19
|
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SHP2-IN-19(compound 183),作为SHP2抑制剂,展现出3 nM的IC50值,主要应用于胶质母细胞瘤研究。 | |||
T81165 |
SHP2-IN-17
|
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SHP2-IN-17(化合物192)作为SHP2抑制剂,具有2 nM的IC50值,适用于胶质母细胞瘤研究。 | |||
T72836 |
SHP2/CDK4-IN-1
|
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SHP2/CDK4-IN-1(化合物10)是一种针对SHP2和CDK4的口服双重抑制剂,具有IC50值分别为4.3和18.2 nM。该化合物能有效引起G0/G1期阻滞,抑制TNBC细胞的增殖,并在EMT6同源小鼠模型中展现出明显的抗肿瘤活性,适用于三阴性乳腺癌(TNBC)的研究。 | |||
T78611 | SHP2-IN-5 | ||
SHP2-IN-5(化合物1)为SHP2抑制剂,IC50为97 nM。SHP2,一种非受体型蛋白酪氨酸磷酸酶,与细胞生长及增殖紧密相关。SHP2-IN-5可能对抑制癌症和其他与SHP2有关的疾病具有治疗潜力。 | |||
T81161 |
SHP2-IN-21
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SHP2-IN-21(化合物208)是一种SHP2抑制剂,其IC50为3 nM,适用于胶质母细胞瘤研究。 | |||
T78694 | SHP2-IN-13 | ||
SHP2-IN-13是一种针对SHP2“tunnel site” 的变构抑制剂,具备高选择性及口服活性,IC50值为83.0 nM。该化合物可作为研究潜力药物,用于治疗携带RTK致癌驱动因素的癌症以及SHP2相关疾病。 | |||
T61701 | SHP2-IN-9 | ||
SHP2-IN-9 is a potent inhibitor (IC50 = 1.174 μM) specifically targeting the SHP2 protein, displaying improved penetration across the blood-brain barrier. It exhibits a remarkable 85-fold selectivity for SHP2 over SHP1. By inhibiting SHP2-mediated cell signal transduction and impairing cancer cell proliferation, SHP2-IN-9 effectively suppresses the growth of both cervix cancer tumors and glioblastoma in vivo [1]. | |||
T81164 |
SHP2-IN-18
|
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SHP2-IN-18(化合物183)作为SHP2抑制剂,具有3 nM的IC50。该化合物适用于胶质母细胞瘤研究。 | |||
T4340 |
SPI-112
|
Phosphatase | Metabolism |
SPI 112 是一种选择性的、有效的、竞争性的SHP2 (PTPN11)抑制剂,对SHP2,蛋白酪氨酸磷酸酶 (PTP) 和 PTP1B 的IC50分别为 1 μM,18.3 μM 和 14.5 μM。 | |||
T13176 |
TNO155
Batoprotafib |
Phosphatase | Metabolism |
TNO155 是具有口服活性野生型SHP2的选择性变构抑制剂 (IC50= 0.011 µM)。它有研究 RTK 依赖性恶性肿瘤(尤其是晚期实体瘤)的潜力。 | |||
T9196 |
IACS-13909
BBP-398 |
Phosphatase | Metabolism |
IACS-13909 (BBP-398) 是具有口服活性的、选择性的 SHP2变构抑制剂,其 IC50=15.7 nM,Kd=32 nM。与其他磷酸酶相比,它对 SHP2的选择性更高。它能够抑制受体酪氨酸激酶 (RTK)/MAPK 途径的信号传导,并具有抗癌作用。 | |||
T28410 |
PHPS1
PHPS-1,PHPS 1 |
Phosphatase | Metabolism |
PHPS1 是 Shp2的选择性抑制剂,对 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的 Ki 分别为 0.73,5.8,10.7,5.8 和 0.47 μM。 | |||
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。 | |||
T68409 |
SHP244
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SHP244 is an allosteric inhibitor of SHP2 with modest thermal stabilization of the enzyme. | |||
T3544 |
SHP099 hydrochloride
|
Phosphatase; Others | Metabolism; Others |
SHP099 hydrochloride 是一种有效的、选择性的、口服生物可利用的、有效的 SHP2 抑制剂。 | |||
T16762 |
RMC-4550
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Phosphatase | Metabolism |
RMC-4550 是选择性的蛋白酪氨酸磷酸酶 2 的变构抑制剂,其IC50=0.583 nM。 | |||
T16350 |
NSC-87877
|
Apoptosis; Phosphatase | Apoptosis; Metabolism |
NSC-87877 是一种Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂,IC50值分别为0.318 μM 和0.355 μM。它还抑制双特异性磷酸酶26。 | |||
T3564 |
SHP099
SHP099 free base,SHP 099,SHP-099 |
Phosphatase; PERK | Apoptosis; Metabolism |
SHP099 (SHP099 free base) free base 是一种选择性的,有效的,有口服活性的 SHP2抑制剂,IC50=70 nM。 | |||
T73552 |
BPDA2
|
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BPDA2为高选择性竞争性SHP2活性位点抑制剂,SHP2的IC50为92.0 nM, 对SHP1及SHP1B的IC50则分别为33.39 μM与40.71 μM。该化合物降低了有丝分裂促进因子、细胞存活信号以及RTK的表达,并抑制了SHP2介导的信号传导,影响乳腺癌细胞表型。 | |||
T4627 |
SPI--112Me
|
Others | Others |
SPI--112Me 是 SPI-112 的前药,在无细胞试验中,它优先抑制 Shp2 的 PTPase 活性超过 Shp1 和 PTP1B 20 倍。 | |||
T6911 |
NSC-87877 disodium
NSC87877 |
Apoptosis; Phosphatase | Apoptosis; Metabolism |
NSC-87877 disodium (NSC87877) 是一种有效的Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂,IC50值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26。 | |||
T16877 |
SHP394
|
Others | Others |
SHP394 is an orally efficacious inhibitor of protein tyrosine phosphatase SHP2 (IC50: 23 nM). | |||
T16878 | SHP836 | Others | Others |
SHP836 is an inhibitor of SHP2 allosteric (IC50: 12 μM for the full-length SHP2). | |||
T39726 |
SHP389
SHP389 |
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SHP389 is an allosteric SHP2 inhibitor, with an IC 50 of 36 nM for both SHP2 and p-ERK. | |||
T39167 |
GS-493
|
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GS-493, a highly specific protein tyrosine phosphatase SHP2 (PTPN11) inhibitor, exhibits remarkable potency with an IC50 of 71 nM. It displays 29- and 45-fold greater affinity towards SHP2 compared to its related counterparts, SHP1 and PTP1B, respectively. In addition, GS-493 impedes both cellular motility and growth of cancer cells, portraying promising antitumor effects. | |||
T25953 |
PHPS1 Sodium
PHPS1 Na,PHPS1 Sodium salt |
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PHPS1 sodium 是 Shp2的选择性抑制剂,对 Shp2,Shp2-R362K,Shp1,PTP1B 和 PTP1B-Q 的Ki 值分别为 0.73,5.8,10.7,5.8 和 0.47 μM。 | |||
T73477 | SHP844 | ||
SHP844为一SHP2抑制剂,IC50值为18.9 µM。SHP2为蛋白酪氨酸磷酸酶(PTP),调控酪氨酸磷酸化水平,影响细胞增殖、分化及存活。 | |||
T69125 |
NSC-13030
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NSC-13030 is a Potent SHP2 Inhibitor with Anti-Proliferative Activity in Breast Cancer Cell Lines | |||
T70919 |
NAT6-297775
|
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NAT6-297775 is a SHP2 inhibitor with IC50 =2.47uM. | |||
T62798 | GDC-1971 | ||
GDC-1971 (compound 199) 是一种 SHP2 的抑制剂。 | |||
T27591 |
II-B08
II-B 08,FAP1 Inhibitor,II-B-08,LMWPTP Inhibitor,Lyp Inhibitor III,CD45 Inhibitor V |
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II-B08 is a cell-permeable SHP2 inhibitor (IC50 = 5.5 µM). II-B08 blocks growth factor stimulated ERK1/2 activation and hematopoietic progenitor proliferation. | |||
T69835 | Plasiatine | ||
Plasiatine is a novel potent activator of the nonreceptor protein tyrosine phosphatase shp2 | |||
T62657 |
SHP504
|
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SHP504 是一种 SHP2 磷酸酶的抑制剂,能够作用于 SHP21–525 (IC50: 21 μM)。 | |||
T39999 |
IACS-15414
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IACS-15414 is a potent SHP2 inhibitor that is effective when administered orally, demonstrating an IC50 value of 122 nM. | |||
T79311 |
CNBCA
|
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CNBCA是一种有效的SHP2酶抑制剂,具有选择性和竞争性,IC50值为0.87 μM。该化合物可结合SHP2全长蛋白并抑制其酶活性,进而阻止Akt和ERK1/2的磷酸化,以及抑制BT474和MDA-MB468乳腺癌细胞的生长。CNBCA主要用于乳腺癌的研究。 | |||
T79123 |
PF-07284892
ARRY-558 |
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PF-07284892 (ARRY-558)作为一种SHP2抑制剂,具有口服活性,其IC50为21 nM,能有效降低pERK表达。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T79985 |
Cryptosporioptide A
|
Phosphatase | Metabolism |
Cryptosporioptide A (Compound 3)是一种从昆虫寄生真菌Cordyceps gracilioides中分离出的色素蛋白酪氨酸磷酸酶抑制剂,针对PTP1B、SHP2、CDC25B、LAR和SHP1等酶展示了抑制作用,其IC50值分别为7.3、5.7、7.6、>50、4.9 μg/mL。 |