T35650
|
|
|
|
Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib trihydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib trihydrochloride has anti-tumor effects[1][2]. |
T68192
|
|
|
|
OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner. |
TN1751
|
|
|
ERK
p38 MAPK
Fatty Acid Synthase
|
(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis. |
T78938
|
|
|
DNA/RNA Synthesis
|
H3B-968为一种高效Werner综合征蛋白(WRN)抑制剂,IC50约为10 nM,可抑制具有解旋酶、ATP酶和外切酶活性的WRN。WRN在癌症研究中具有显著的合成致死潜力。H3B-968通过与ATP竞争抑制WRN解旋酶活性。 |
T63287
|
|
|
|
HPK1-IN-3 是一种选择性的、有效的、ATP 竞争性的造血祖细胞激酶 1 (HPK1; MAP4K1) 抑制剂 (IC50: 0.25 nM)。HPK1-IN-3 具有 IL-2 细胞效力,能够作用于人外周血单核细胞 (PBMC),EC50 值为 108 nM。 |
T68341
|
|
|
|
HS56 是一种 ATP 竞争性 Pim/DAPK3双重抑制剂,对 DAPK3、Pim-3、Pim-1和 Pim-2 的 Ki 值分别为 0.26、0.208、2.94 和 >100 μM。 HS56 抑制 LC20 磷酸化和平滑肌收缩。HS56 降低自发性高血压小鼠的血压。HS56可用于高血压研究。 |
T12068
|
|
|
Others
|
MK-8033 hydrochloride 是一种有效的、具有口服活性的 ATP 竞争性 c-Met/Ron 双重抑制剂 ,对c-Met 的为1 nM ,对Ron 的IC50为7nM。MK-8033 hydrochloride 对活化的激酶构象 (activated kinase conformation)具有很高的亲和力,可用于乳腺癌,膀胱癌、非小细胞肺癌 (NSCLC)等癌症的研究。 |
T9684
|
|
|
|
(Z)-Orantinib ((Z)-SU6668) 是一种有效,选择性,具有口服活性和 ATP 竞争性的 Flk‐1/KDR,PDGFRβ和 FGFR1抑制剂,IC50值分别为 2.1,0.008 和 1.2 μM。(Z)-Orantinib 是有效的抗血管生成和抗肿瘤剂,可诱导已形成的肿瘤消退。 |
T36672
|
|
|
|
The extracellular signal-regulated kinase (ERK) signal transduction pathway regulates a diverse array of cellular processes. These processes include cell survival, proliferation, motility, and differentiation and are constitutively activated in cancers involving lung, colon, pancreas, kidney, and ovary. CAY10561 is a potent, ATP-competitive inhibitor of ERK2 (Ki = 2 nM). This compound is highly selective for ERK2 compared to other kinases such as PKA (Ki = 0.39 μM) and JNK3 (Ki = 4 μM). CAY10561 inhibits proliferation of COLO 205 cells with an IC50 value of 0.54 μM. |
T69055
|
|
|
|
PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2). |