SKLB325 是一种JMJD6抑制剂，其结合亲和力 (KD) 值为 0.755 μM，IC50值为 0.7797 μM。SKLB325 在体内外对卵巢癌均显示抗肿瘤作用。SKLB325 诱导细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。SKLB325 在肾细胞癌 (RCC) 中表现出显着的抗肿瘤功效。

SKLB325 is a Jumonji domain-containing 6 ( JMJD6 ) inhibitor with a binding affinity ( K D ) value of 0.755 μM, and the IC 50 value of 0.7797 μM. SKLB325 shows antitumor effects on ovarian cancer both in vivo and in vitro. SKLB325 induces apoptosis [1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2].

SKLB325 inhibits ovarian cancer growth through inhibition of proliferation and induction of apoptosis and cell death, and inhibiting angiogenesis may play a significant role in inhibiting tumor growth [1]. SKLB325 (0.25-16 μM; for 24-72 h) has significant inhibitory effects on the in vitro proliferation of ovarian cancer cells. Furthermore, the most effective concentration at which JMJD6 inhibited SKOV3 cell growth is 4 μM, and the optimal duration of action is 72 h [1]. SKLB325 upregulates the expression of p53 and its downstream effectors at both the mRNA and protein levels in vitro [1]. Cell Proliferation Assay [1] Cell Line: SKOV3, ES2, A2780s and CP70 cells Concentration: 0, 0.25, 0.5, 1, 2, 4, 8, and 16 μM Incubation Time: 24 h, 48 h, and 72 h Result: With increasing SKLB325 concentration, the inhibitory effect also increased, exhibiting a significant dose-response relationship. There was a significant difference between the drug group across different doses and the control group. Western Blot Analysis [1] Cell Line: SKOV3, ES2 and A2780s cells Concentration: 4 μM Incubation Time: 72 hours Result: p53, p21, and PUMA protein levels were significantly upregulated in SKOV3, ES2 and A2780s cells.

SKLB325 (10 mg/kg) shows antitumor activities in an intraperitoneal xenograft model. SKLB325 significantly prolongs the survival of tumor-bearing mice without obvious side effects. SKLB325 treatment protocols were effective in suppressing SKOV3, ES2, CP70, and A2780s tumor growth in nude mice [1]. Animal Model: Female athymic BALB/c nude mice [1] Dosage: 10 mg/kg Administration: I.p. injections every three days for eight doses total Result: The average weight of intraperitoneal tumor nodules was 1.56 ± 0.70, 1.04 ± 0.62, and 0.14 ± 0.11 g in the control, vehicle and SKLB325 groups, respectively. Tumor weight was significantly reduced by 91 and 86% in the SKLB325 groups compared to the control and vehicle groups, respectively.

C12H12N4O2

244.25

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years