2408842-51-1
2408842-51-1 structure
- Name: WDR5-IN-1
- Chemical Name: WDR5-IN-1
- CAS Number: 2408842-51-1
- Molecular Formula: C30H31FN4O3
- Molecular Weight: 514.59
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2020-04-10 15:32:08
- Modify Date: 2024-01-15 00:16:24
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WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1].
| Name | WDR5-IN-1 |
|---|
| Description | WDR5-IN-1 is a potent and selective WD repeat domain 5 (WDR5) inhibitor, with a Kd of <0.02 nM. WDR5-IN-1 inhibits MLL1 histone methyltransferase (HMT) activity with an IC50 of 2.2 nM. WDR5-IN-1 diminishes MYC recruitment at WDR5-displaced genes and exhibits potent anti-proliferative effects in CHP-134 (neuroblastoma) and Ramos (Burkitt’s lymphoma) lines[1]. |
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| Related Catalog | |
| In Vitro | WDR5-IN-1 (1 µM; 48 hours) shows an apparent decrease in G2M phase cells[1]. WDR5-IN-1 (0.01-3 µM; 24-48 hours) increases p53 and p21 protein levels[1].WDR5-IN-1 shows anti-proliferative activity in MYC-driven cancers (CHP-134, Ramos, Raji, Daudi, SW620, SW480 cells), with GI50s ranging from 0.26-3.2 µM[1]. Cell Cycle Analysis[1] Cell Line: MV4:11 cells Concentration: 1 µM Incubation Time: 48 hours Result: Showed an approximate 4 fold increased SubG1 cells. Western Blot Analysis[1] Cell Line: MV4:11 cells Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3 µM Incubation Time: 24, 48 hours Result: p53 and p21 protein levels started to increase from 8 h post treatment of compound 16 at 300 nM and continued to elevate up to 32 h. |
| References |
| Molecular Formula | C30H31FN4O3 |
|---|---|
| Molecular Weight | 514.59 |