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JQAD1

  Cat. No.:  DC72756   Featured
Chemical Structure
2417097-18-6
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More than 5000 active chemicals with high quality for research!
Field of application
JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2417097-18-6
Chemical Name: JQAD1
Synonyms: JQAD1
SMILES: O=C1N(C(=O)O[C@]21CCC1=CC(NC(=O)CCCCCCCCCCCNC3=CC=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=C3)=CC=C21)CC(=O)N([C@@H](C)C(F)(F)F)CC1C=CC(F)=CC=1
Formula: C48H52F4N6O9
M.Wt: 932.954906463623
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer.
In Vivo: JQAD1 (40 mg/kg; i.p.; once daily, for 21 days) inhibits tumor growth in NSG mice with Kelly NB cell xenografts [1]. It also prolongs survival in these mice. In another study using CD1 mice, JQAD1 was administered at a dosage of 10 mg/kg via intraperitoneal injection for pharmacokinetic analysis [1]. The results showed that JQAD1 had a half-life of 13.3 hours (±3.37 SD) in murine serum and reached a maximum concentration (Cmax) of 7 μmol/L.
In Vitro: JQAD1 inhibits the expression of EP300, suppresses H3K27ac modification, and induces apoptosis in Kelly NB cells (control group) rather than CRBN knockout cells [1]. Treatment with JQAD1 (0.5 or 1 μM; 6-96 hours) leads to early time-dependent induction of the sub G1 peak, indicating apoptosis in Kelly and NGP cells [1]. JQAD1 (1 μM; 12-36 hours) induces apoptosis in Kelly NB cells [1]. Cells treated with JQAD1 (0.5 μM; 24 hours) show upregulation of pro-apoptotic BH3 effectors BIM, BID, and PUMA, as well as pro-apoptotic mediators BAX, along with the upregulation of their inhibitors BCL2 and MCL1 [1]. JQAD1 (0.5 and 1 μM; 24 hours) disrupts MYCN expression [1]. JQAD1 (0.5 μM; 24 hours) results in loss of H3K27ac on chromatin [1]. JQAD1 (1.2 nM - 20 μM; 5 days) exhibits broad CRBN-dependent anti-tumor activity across cancer cell lines [1]. JQAD1 induces time-dependent degradation of EP300, observed as early as 16 hours [1]. Western Blot Analysis [1]: Cell Line: MYCN-amplified neuroblastoma (NB) cells Concentration: 0.1, 0.5, 1, 3, 5, and 10 µM Incubation Time: 24 hours Result: Demonstrated a dose-dependent decrease in EP300 expression, accompanied by a parallel loss of the H3K27ac modification. Induced selective loss of EP300 expression coincided with cleavage of PARP1, indicating the initiation of apoptosis. Western Blot Analysis [1]: Cell Line: Kelly NB cells Concentration: 1 µM Incubation Time: 12, 24, and 36 hours Result: Increased expression of cleaved caspase-3 and cleaved PARP1 in a dose-dependent manner.
References: [1]. Durbin AD, et, al. EP300 Selectively Controls the Enhancer Landscape of MYCN-Amplified Neuroblastoma. Cancer Discov. 2022 Mar 1;12(3):730-751.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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