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59

抑制剂 & 化合物

1

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Cat. No. Product Name Target Signaling Pathways
T40121 SHP2-D26

SHP2-D26

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

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

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

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

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

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

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

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

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

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

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

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 Shp2Shp2-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

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

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Shp2Shp1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

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Shp2Shp1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

SHP389 is an allosteric SHP2 inhibitor, with an IC 50 of 36 nM for both SHP2 and p-ERK.
T39167 GS-493

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

PHPS1 sodium 是 Shp2的选择性抑制剂,对 Shp2Shp2-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

NSC-13030 is a Potent SHP2 Inhibitor with Anti-Proliferative Activity in Breast Cancer Cell Lines
T70919 NAT6-297775

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

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

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

IACS-15414 is a potent SHP2 inhibitor that is effective when administered orally, demonstrating an IC50 value of 122 nM.
T79311 CNBCA

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

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。

化合物

SHP2-D26
Cat.No: T40121
Synonym: SHP2-D26
Target:
JAB-3068
Cat.No: T39640
Synonym: SHP2-IN-6
Target: Phosphatase
SHP2 protein degrader-1
Cat.No: T40250
Synonym: SHP2 protein degrader-1
Target:
RMC-4630
Cat.No: T39658
Synonym: SHP2-IN-7,RMC-4630
Target: Phosphatase
SHP2-IN-6 hydrochloride
Cat.No: T39641
Synonym: SHP2-IN-6 hydrochloride
Target:
SHP2 IN-1
Cat.No: T12903
Synonym:
Target: Others
SHP2 inhibitor LY6
Cat.No: T63993
Synonym:
Target:
SHP2-IN-20
Cat.No: T81162
Synonym:
Target:
SHP2-IN-14
Cat.No: T79108
Synonym:
Target:
SHP2 protein degrader-2
Cat.No: T74430
Synonym:
Target:
SHP2-IN-8
Cat.No: T61891
Synonym:
Target:
SHP2-IN-16
Cat.No: T79412
Synonym:
Target:
SHP2-IN-22
Cat.No: T78896
Synonym:
Target:
SHP2/HDAC-IN-1
Cat.No: T72839
Synonym:
Target:
SHP2-IN-19
Cat.No: T81163
Synonym:
Target:
SHP2-IN-17
Cat.No: T81165
Synonym:
Target:
SHP2/CDK4-IN-1
Cat.No: T72836
Synonym:
Target:
SHP2-IN-5
Cat.No: T78611
Synonym:
Target:
SHP2-IN-21
Cat.No: T81161
Synonym:
Target:
SHP2-IN-13
Cat.No: T78694
Synonym:
Target:
SHP2-IN-9
Cat.No: T61701
Synonym:
Target:
SHP2-IN-18
Cat.No: T81164
Synonym:
Target:
SPI-112
Cat.No: T4340
Synonym:
Target: Phosphatase
TNO155
Cat.No: T13176
Synonym: Batoprotafib
Target: Phosphatase
IACS-13909
Cat.No: T9196
Synonym: BBP-398
Target: Phosphatase
PHPS1
Cat.No: T28410
Synonym: PHPS-1,PHPS 1
Target: Phosphatase
Bis(maltolato)oxovanadium(IV)
Cat.No: T22276
Synonym: 双(麦芽醇)氧钒(IV),BMOV,Bis maltolato oxovanadium,Bis(maltolato)oxovanadium (IV),bis maltolato oxo vanadium,Bis(maltolato)oxovanadium (IV)
Target: Phosphatase, Others
SHP244
Cat.No: T68409
Synonym:
Target:
SHP099 hydrochloride
Cat.No: T3544
Synonym:
Target: Phosphatase, Others
RMC-4550
Cat.No: T16762
Synonym:
Target: Phosphatase
NSC-87877
Cat.No: T16350
Synonym:
Target: Apoptosis, Phosphatase
SHP099
Cat.No: T3564
Synonym: SHP099 free base,SHP 099,SHP-099
Target: Phosphatase, PERK
BPDA2
Cat.No: T73552
Synonym:
Target:
SPI--112Me
Cat.No: T4627
Synonym:
Target: Others
NSC-87877 disodium
Cat.No: T6911
Synonym: NSC87877
Target: Apoptosis, Phosphatase
SHP394
Cat.No: T16877
Synonym:
Target: Others
SHP836
Cat.No: T16878
Synonym:
Target: Others
SHP389
Cat.No: T39726
Synonym: SHP389
Target:
GS-493
Cat.No: T39167
Synonym:
Target:
PHPS1 Sodium
Cat.No: T25953
Synonym: PHPS1 Na,PHPS1 Sodium salt
Target:
SHP844
Cat.No: T73477
Synonym:
Target:
NSC-13030
Cat.No: T69125
Synonym:
Target:
NAT6-297775
Cat.No: T70919
Synonym:
Target:
GDC-1971
Cat.No: T62798
Synonym:
Target:
II-B08
Cat.No: T27591
Synonym: II-B 08,FAP1 Inhibitor,II-B-08,LMWPTP Inhibitor,Lyp Inhibitor III,CD45 Inhibitor V
Target:
Plasiatine
Cat.No: T69835
Synonym:
Target:
SHP504
Cat.No: T62657
Synonym:
Target:
IACS-15414
Cat.No: T39999
Synonym:
Target:
CNBCA
Cat.No: T79311
Synonym:
Target:
PF-07284892
Cat.No: T79123
Synonym: ARRY-558
Target:
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。

天然产物

Cryptosporioptide A
Cat.No: T79985
Synonym:
Target: Phosphatase
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