JH-XI-10-02
CAS No. : 2209085-22-1
| Size | Price | Stock |
|---|---|---|
| 1mg | $370 | In-stock |
| 5mg | $1180 | In-stock |
| 10mg | $1890 | In-stock |
| 25mg | $3780 | In-stock |
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| 100 mg | Get quote | |
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| Cat. No. : | HY-111518 |
| M.Wt: | 920.14 |
| Formula: | C53H69N5O9 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
JH-XI-10-02 is a PROTAC connected by ligands for Cereblon and CDK. JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19[1]. IC50 & Target:IC50: 159 nM (CDK8)[1] In Vitro: JH-XI-10-02, a bivalent small molecule degrader, recruits the E3 ligase CRL4Cereblon to promote the ubiquitination and proteosomal degradation of CDK8[1].
JH-XI-10-02 (1 μM) induces partial degradation of CDK8 in Jurkat cells upon treatment for 6 h. JH-XI-10-02 (1 μM) induces significant degradation of CDK8 after treatment for 24 h[1].
JH-XI-10-02 induces degradation of CDK8 at 5 μM in WT Molt4 cells, no degradation in CRBN Molt4 cells at any concentration (0.1-5 μM) in WT Molt4 cells and Molt4 cells where CRBN had been subject to CRISPER/CAS9-mediated deletion for 24 h[1].
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