Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T6120 |
Pralatrexate
Folotyn,10-炔丙基-10-去氮杂氨基蝶呤,10-Propargyl-10-deazaaminopterin,普拉曲沙 |
Apoptosis; DHFR; Antifolate; TAM Receptor | Apoptosis; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism; Tyrosine Kinase/Adaptors |
Pralatrexate (10-Propargyl-10-deazaaminopterin) 是一种抗叶酸剂,也是二氢叶酸还原酶抑制剂,Ki 值为 13.4 pM。它具有抗肿瘤活性,可研究复发/难治性 T 细胞淋巴瘤。它是叶酰聚谷氨酸合成酶的底物,具有改善的细胞摄取和保留能力。 | |||
T7265 |
HSP27 inhibitor J2
J2 |
HSP | Cytoskeletal Signaling; Metabolism |
HSP27 inhibitor J2 (J2) 是一种HSP27抑制剂,可显著增强 17-AAG 的抗增殖活性,并对顺铂诱导的肺癌细胞生长抑制具有敏感性。它显著诱导异常 HSP27 二聚体形成并抑制HSP27巨聚合物的产生,从而具有抑制HSP27的伴侣功能和降低细胞保护功能的作用。 | |||
T82566 |
DiaPep277
|
||
DiaPep277为源自HSP60第437-460位点的24个氨基酸组成的多肽,能够抑制NOD小鼠β-细胞破坏进展,并在糖尿病动物模型中对T细胞表现出免疫调节功能。 | |||
T78728 |
SP27
|
PROTACs | PROTAC |
SP27为一种选择性PROTAC,专一地降解PLK4,具有19.5 nM的DC50。该化合物主要应用于乳腺癌研究。 | |||
T82683 |
Connexin mimetic peptide 40GAP27
|
||
Connexin mimetic peptide 40GAP27 是一种生物活性肽,对应于主要的血管连接蛋白Cx40第二个细胞外环的GAP27结构域(40Gap27)。该化合物在研究氧化应激所致的损伤以及间隙连接通讯机制中有应用。40Gap27能够在给药后减少内皮依赖性的内膜下平滑肌的超极化现象。 | |||
T4253 |
Skp2 Inhibitor C1
SKPin C1 |
Others; E1/E2/E3 Enzyme | Others; Ubiquitination |
Skp2 Inhibitor C1 (SKPin C1)(SKPin C1)是Skp2介导p27降解的特异性抑制剂。 | |||
T16889 |
SJ572403
SJ403 |
Others | Others |
SJ572403 是一种无序蛋白 p27 的抑制剂,对于 p27-KID 的 D2 亚结构域内的特定区域的 Kd 为 2.2 mM。 SJ572403 可用于研究具有内在无序蛋白质的疾病。 | |||
T13349 |
WS-383
|
E1/E2/E3 Enzyme | Ubiquitination |
WS-383 是高效、选择性、可逆的DCN1-UBC12相互作用抑制剂,IC50为11 nM。它抑制 Cul3/1 的类泛素化修饰,引起 NRF2,p21和p27 的积累。 | |||
T13244 |
Ubiquitination-IN-1
|
Others | Others |
Ubiquitination-IN-1 是一种有效的泛素化和Cksl-Skp2蛋白互作抑制剂 (IC50=0.17 μM) 抑制剂,增加 p27 水平,可通过阻断肿瘤抑制因子的降解发挥作用。 | |||
T3317 |
SZL P1-41
|
Apoptosis; Others; E1/E2/E3 Enzyme | Apoptosis; Others; Ubiquitination |
SZL P1-41 是 Skp2 抑制剂,可以阻止 Skp2-Skp1 复合物的组装。 它选择性地抑制 Skp2 SCF E3 连接酶活性,还在体内外抑制 Skp2 介导的 p27 和 Akt 泛素化。 它通过触发细胞衰老和抑制糖酵解来抑制 Y 细胞和 Y 干细胞的存活,有抗肿瘤作用。 | |||
T9229 |
Pim-1/2 kinase inhibitor 1
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
Pim-1/2 kinase inhibitor 1 是一种具有口服活性的 Pim-1/2 激酶抑制剂。Pim-1/2 kinase inhibitor 1 能阻断 Pim 激酶磷酸化肽的能力,并且抑制4E-BP1和p27Kip1的Pim 蛋白激酶定向磷酸化。Pim-1/2 kinase inhibitor 1 可用于癌症,尤其是前列腺癌的研究。 | |||
T25738 |
Linichlorin A
Elegin |
||
Linichlorin A is used as a p27(Kip1) ubiquitination inhibitor. | |||
T71864 |
SJ572710
|
||
SJ572710 is an inhibitor of the disordered protein, p27(Kip1). | |||
T68845 | Americanin A | ||
Americanin A natural thrombin inhibitor, suppressing melanin synthesis, regulating the ATM/ATR signaling pathway and the Skp2-p27 axis in human colon cancer cells. | |||
T71830 |
DT204
|
||
DT204 is a SCFSkp2 inhibitor which blocks Skp2 binding to Cullin-1 and Commd1, thereby synergistically enhancing BTZ-induced apoptosis and stabilization. DT204 also increases p27 levels. | |||
T11396 |
GGTI-2418
|
Transferase | Metabolism |
GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors. GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. | |||
T72522 |
Aurora kinase-IN-1
|
||
Aurora kinase-IN-1 是aurora kinase 的有效抑制剂。Aurora kinase-IN-1 上调 G1 细胞周期抑制蛋白 (包括 p21 和 p27) 以及 G1 进行性细胞周期蛋白 D1 的表达,并下调 G1-to-S 进行性细胞周期蛋白,导致细胞周期停滞在 G1/S 边界。Aurora 激酶-IN-1 还诱导细胞凋亡 (apoptosis)。Aurora 激酶-IN-1 是化疗药物的先导化合物。 | |||
T13292 | VDR agonist 1 | Others | Others |
VDR agonist 1 (compound 28) 是一种非甾体类维生素 D 受体 (VDR)的激动剂, 在MCF-7 细胞中测得其IC50值为 690 nM。VDR agonist 1 通过上调 p21 和 p27 的表达来抑制细胞周期,通过增加 BAX 的表达来促进细胞凋亡,降低 Bcl-2 的表达,具有治疗乳腺癌的潜力。 | |||
T29172 |
YD277
YD 277,YD-277 |
||
YD277 is a small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibitio | |||
T69200 | CGP74514A | ||
CGP74514A is a CDK1 inhibitor with potential anticancer activity. In U937 cells, CGP74514A - induced apoptosis (5 microM) became apparent within 4 hr and approached 100% by 24 hr. The pan- caspase inhibitor Boc-fmk and the caspase-8 inhibitor lETD-fmk opposed CGP74514A -induced caspase-9 activation and PARP degradation, but not cytochrome c or Smac/DIABLO release. CGP74514A -mediated apoptosis was substantially blocked by ectopic expression of full-length Bel- 2, a loop-deleted mutant Bcl-2, and... | |||
T70962 | MHY219 | ||
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M... |