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MedChemExpress - Model SKLB325 -66680-03-3

SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755?μM, and the IC50 value of 0.7797?μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis[1]. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) [2].

SKLB325

MCE China：SKLB325

Brand：MedChemExpress (MCE)

Cat. No.HY-139782

CAS：66680-03-3

Purity：99.23%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755?μM, and the IC50 value of 0.7797?μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis. SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .

In Vitro：SKLB325 suppresses 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].

In Vivo：SKLB325 (10?mg/kg) has 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].

References：

[1]. Heng Zheng, et al. Jumonji domain-containing 6 (JMJD6) identified as a potential therapeutic target in ovarian cancer. Signal Transduct Target Ther.2019 Jul 26;4:24. [Content Brief]

[2]. Chuanjie Zhang, et al. Epigenome screening highlights that JMJD6 confers an epigenetic vulnerability and mediates sunitinib sensitivity in renal cell carcinoma. Clin Transl Med. 2021 Feb;11(2):e328. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。

MedChemExpress - Model SKLB325 -66680-03-3

MCE products for research use only. We do not sell...

SKLB325