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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3032 |
VE-821
ATR Inhibitor IV |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
VE-821 (ATR Inhibitor IV) 是一种有效的 ATP 竞争性的ATR 抑制剂,Ki 为 13 nM,IC50为 26 nM。 | |||
T1821 |
CGK733
CGK 733 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
CGK733 (CGK 733) 是一种有效的选择性 ATM/ATR 抑制剂,用于癌症研究。 | |||
T5175 |
azd1390
|
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZD1390 是一种可口服的,可渗透脑的ATM 高度选择性抑制剂,IC50为 0.78 nM。 | |||
T6770 |
AZD0156
|
Apoptosis; ATM/ATR | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZD0156 是一种口服活性 ATM 选择性抑制剂,IC50为 0.58 nM。它抑制 ATM 介导的信号转导,防止 DNA 损伤检查点激活,破坏 DNA 损伤修复,起抗肿瘤作用。 | |||
T2685 |
KU-55933
ATM Kinase Inhibitor |
ATM/ATR; DNA-PK; PI3K; mTOR; Autophagy | Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
KU-55933 (ATM Kinase Inhibitor) 是一种 ATM 抑制剂,IC50和 Ki 值分别为 12.9 和 2.2 nM。它对 ATM 的选择性比对 PI3K/PI4K、 DNA-PK、ATR 和 mTOR 高。 | |||
T6261 |
CP-466722
CP 466722,CP466722 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
CP-466722 是一种有效且可逆的 ATM 抑制剂,IC50值为 4.1 μM。它不会抑制细胞中的 ATR 和 PI3K 或 PIKK 家族成员。 | |||
T6612 |
NU6027
|
ATM/ATR; DNA-PK; CDK | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
NU6027 是一种有效的 ATR/CDK 抑制剂,抑制 CDK1/2、ATR 和 DNA-PK,Ki 为 2.5 μM/1.3 μM、0.4 μM 和 2.2 μM。它以 ATR 依赖性方式增强羟基脲和顺铂的细胞毒性。 | |||
T1958 |
AZ20
|
ATM/ATR; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZ20 是一种有效且特异性的 ATR 激酶抑制剂,IC50值为 5 nM。它还抑制mTOR 活性,IC50值为 38 nM。 | |||
T4443 |
AZ32
|
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZ32 是一种口服生物利用度和血脑屏障穿透性 ATM 抑制剂,对 ATM 酶的 IC50 <6.2 nM,对细胞内 ATM 的 IC50 为 0.31 μM。 | |||
T3338 |
Ceralasertib
AZD6738 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Ceralasertib (AZD6738) 是一种具有口服活性的选择性 ATR 激酶抑制剂,IC50 为 1 nM。 | |||
T2084 |
ETP-46464
|
ATM/ATR; DNA-PK; PI3K; mTOR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
ETP-46464 是一种有效且特异性的 ATR 抑制剂,IC50为 25 nM。 | |||
T7122 |
AZD-7648
|
DNA-PK | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZD-7648 是一种 DNA 依赖性蛋白激酶 (DNA-PK) 抑制剂,在酶试验中 IC50 为 0.63 nM,具有抗肿瘤活性。 | |||
T7318 |
Elimusertib
BAY-1895344 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Elimusertib (BAY-1895344) 是一种可口服的选择性ATR 抑制剂,IC50值为 7 nM。它具有抗肿瘤活性,可研究实体瘤和淋巴瘤。 | |||
T1923 |
BRD4770
|
Histone Methyltransferase | Chromatin/Epigenetic |
BRD4770 是组蛋白甲基转移酶G9a 抑制剂,可激活共济失调毛细血管扩张突变途径并诱导细胞衰老。它可抑制H3K9的二甲基和三甲基化,EC50为 5 µM。 | |||
T6100 |
Torin 2
|
Apoptosis; ATM/ATR; DNA-PK; mTOR; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Torin 2 是一种特异性 mTOR 抑制剂,IC50值为0.25 nM,并改善了药代动力学特性。它抑制 ATM/ATR/DNA-PK 的 EC50 分别为 28 nM/35 nM/118 nM。 | |||
T15673 |
KU 59403
KU-59403,KU59403 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
KU 59403 是一种具有选择性和高效性的 ATM 抑制剂,具有抗肿瘤和抗癌活性,抑制 ATM、DNA-PK 和 PI3K,常与PARP或ATR抑制剂的联合治疗来延缓癌症的进程。 | |||
T62083 |
Camonsertib
ATR inhibitor 4,RP-3500 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Camonsertib (RP-3500) 是一种选择性的、口服具有活力的 ATR 激酶抑制剂 (ATRi),在生化试验中的 IC50: 1.00 nM,表现出有效的抗肿瘤作用。RP-3500 对 ATR 的选择性是 mTOR 的 30 倍 (IC50: 120 nM),是 ATM、DNA-PK 和 PI3Kα 激酶的 2,000 倍以上。 | |||
T19671 |
AZ31
AZ 31,AZ-31 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
AZ31 是一种 ATM 抑制剂,具有有效性、高选择性、和口服活性。AZ31对 ATM 酶、细胞内 ATM 具有抑制作用,IC50 值 分别为<1.2 nM 和 46 nM。AZ31 表现出优异的 ATR 选择性 、PIKK 家族选择性和泛激酶选择性。AZ31 是一种强效的体外放射增敏剂,可用于研究癌症。 | |||
T2433 |
NU 7026
NU7026,DNA-PK Inhibitor II,LY293646 |
Apoptosis; ATM/ATR; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
NU 7026 (DNA-PK Inhibitor II) 是一种新型特异性的DNA-PK 抑制剂,IC50为 0.23 μM,也抑制PI3K,IC50为 13 μM。 | |||
T68845 |
Americanin A
|
Others | Others |
Americanin A natural thrombin inhibitor, suppressing melanin synthesis, regulating the ATM/ATR signaling pathway and the Skp2-p27 axis in human colon cancer cells. | |||
T73301 |
ATR-IN-20
|
Others | Others |
ATR-IN-20是一种高效的ATR(ATM/ATR)抑制剂, IC50值仅为3 nM。该化合物还能抑制mTOR(IC50值为18 nM),并展示出对PI3Kα(100 nM)、ATM(100 nM)和DNA-PK(662 nM)的良好选择性。ATR-IN-20具备优秀的药代动力学属性(F=30%),同时显示了其抗癌潜力。 | |||
T62290 |
SKLB-197
|
Others | Others |
SKLB-197 能够作用于 ATR (IC50: 0.013 μM),但对其他 402 种蛋白激酶的活性极弱或无活性。在体外和体内,SKLB-197 对 ATM 缺陷型肿瘤具有显著的抗肿瘤作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TN1673 |
Garcinone C
伽升沃 C,伽升沃C |
ATM/ATR; CDK; STAT; AChR; Antifection | Cell Cycle/Checkpoint; DNA Damage/DNA Repair; JAK/STAT signaling; Microbiology/Virology; Neuroscience; PI3K/Akt/mTOR signaling; Stem Cells |
Garcinone C 是一种从 Garcinia oblongifolia Champ 中提取的黄酮衍生物,具有抗炎、收敛和促进肉芽的活性。 Garcinone C 是一种 AChE 抑制剂,对某些癌症具有潜在的细胞毒性作用。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPY-02953 |
TEM8/ANTXR1 Protein, Human, Recombinant (hFc)
ATR,TEM8,anthrax toxin receptor 1,GAPO |
Human | HEK293 Cells |
ANTXR1 contains 1 VWFA domain and belongs to the ATR family. ATR (Ataxia telangiectasia and Rad3 related) and ATM (Ataxia telangiectasia mutated) are closely related kinases that are activated by DNA damage. They are serine-threonine protein kinases and belongs to the phosphatidylinositol 3' kinase-like kinase (PIKK) family. Upon recruitment by the DNA damage binding proteins/complexes (ATRIP for ATR; MRN for ATM), ATM/ATR initiate the DNA damage checkpoint by phosphorylating a number of key pro... | |||
TMPY-03976 |
EEF1E1 Protein, Human, Recombinant (His)
eukaryotic translation elongation factor 1 ε 1,P18,eukaryoti... |
Human | E. coli |
EEF1E1, also known as AIMP3 and p18, is a multifunctional protein that localizes to both the cytoplasm and nucleus. In the cytoplasm, EEF1E1 is an auxiliary component of the macromolecular aminoacyl-tRNA synthase complex. It is comprised of a bifunctional glutamyl-prolyl-tRNA synthase, the monospecific isoleucyl, leucyl, glutaminyl, methionyl, lysyl, arginyl and aspartyl-tRNA synthases, and three auxiliary proteins, EEF1E1/p18, AIMP2/p38 and AIMP1/p43. EEF1E1 also plays a positive role in ATM/AT... | |||
TMPJ-00870 |
NCK1 Protein, Human, Recombinant (His)
SH2/SH3 Adaptor Protein NCK-α,SH2/SH3 Adaptor Protein NCK-Al... |
Human | E. coli |
Cytoplasmic Protein NCK1 (NCK1) is a cytoplasmic protein that contains one SH2 domain and three SH3 domains. NCK1 is a member of the adapter family, which associates with tyrosine-phosphorylated growth factor receptors, such as KDR and PDGFRB, or their cellular substrates. NCK1 maintains low levels of EIF2S1 phosphorylation by promoting its dephosphorylation by PP1. NCK1 plays a role in the DNA damage response, but not in the detection of the damage by ATM/ATR. It is also involved in transducing... | |||
TMPY-02228 |
p53 Protein, Cynomolgus, Recombinant
tumor protein p53,p53,TP53 |
Cynomolgus | E. coli |
p53, also known as Tp53, is a DNA-binding protein which belongs to the p53 family. It contains transcription activation, DNA-binding, and oligomerization domains. p53 protein is expressed at low level in normal cells and at a high level in a variety of transformed cell lines, where it's believed to contribute to transformation and malignancy. p53 (TP53) is a transcription factor whose protein levels and post-translational modification state alter in response to cellular stress (such as DNA damag... |