CC-90009

  Cat. No.:  DC28693   Featured
Chemical Structure
1860875-51-9
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Field of application
CC-90009 is a cereblon modulator. CC-90009 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3), which are transcriptional repressors in T-cells. This reduces the levels of these transcription factors, and modulates the activity of the immune system, which may include the activation of T-lymphocytes. .
Cas No.: 1860875-51-9
Chemical Name: Eragidomide
Synonyms: Cereblon modulator 1;BCP33889;CC90009; CC 90009; Cereblon modulator 1;2-(4-chlorophenyl)-N-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)-2,2-difluoroacetamide;Eragidomide
SMILES: ClC1C([H])=C([H])C(=C([H])C=1[H])C(C(N([H])C([H])([H])C1C([H])=C([H])C2C(N(C([H])([H])C=2C=1[H])C1([H])C(N([H])C(C([H])([H])C1([H])[H])=O)=O)=O)=O)(F)F
Formula: C22H18ClF2N3O4
M.Wt: 461.8458
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Cereblon modulator 1 (compound F) is a cereblon (CRBN) E3 ligase modulator. Cereblon modulator 1 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3)[1][2].
Target: Cereblon
In Vitro: A different CRBN-binding compound, Cereblon modulator 1 (compound F), that demonstrates anti-proliferative activity in non-AML hematological cancer cell lines (such as multiple myeloma) does not inhibit cell growth in any of the 11 AML cell lines tested, including the ten cell lines that are sensitive to the growth inhibitory activity of Compound D. However, when excess Cereblon modulator 1 is added to KG-1 AML cell cultures in the presence of Compound D, the anti-proliferative activity of Compound D is reduced, presumably due to competition for binding of Compound D to CRBN. The relative impact of Cereblon modulator 1 on the anti-proliferative effect of Compound D progressively increased with increasing concentrations of Cereblon modulator 1. In the presence of 100 µΜ Cereblon modulator 1, the potency of Compound D in inhibiting cell growth reduced by approximately 60-fold, and the potency of Compound D in inducing apoptosis reduced by approximately 40-fold[1].
References: [1]. Ellen Filvaroff, et al. Methods for treating cancer and the use of biomarkers as a predictor of clinical sensitivity to therapies. WO2017120446A1. [2]. CC-90009
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC39709 Lenalidomide-Br Lenalidomide-Br (Compound 41) is an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, and is used in the recruitment of CRBN protein. Lenalidomide-Br can be connected to the ligand for protein by a linker to form PROTACs.
DC72888 Z0933M Z0933M is a potent S phase kinase-associated protein 1 (Skp1) inhibitor with Kd of 54 nM, potently inhibits Skp1-F-box protein-protein interactions with Ki value of 231 nM in FP-based in vitro competition assays.
DC72103 CC-99282 CC-99282 (Golcadomide) is an orally active cereblon (CRBN) E3 ligase modulator (CELMoD). Ikaros and Aiolos are degraded potently and specifically by CC-99282, which co-opts CRBN.
DC42464 CRBN modulator-1 CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
DC28693 CC-90009 CC-90009 is a cereblon modulator. CC-90009 specifically binds to CRBN, thereby affecting the activity of the ubiquitin E3 ligase complex. This leads to the ubiquitination of certain substrate proteins and induces the proteasome-mediated degradation of certain transcription factors, including Ikaros (IKZF1) and Aiolos (IKZF3), which are transcriptional repressors in T-cells. This reduces the levels of these transcription factors, and modulates the activity of the immune system, which may include the activation of T-lymphocytes. .
DC11579 VH032 VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM..
DC11565 E3 Ligase Ligand 2 E3 ligase Ligand 2 is a Ligand for E3 Ligase used in PROTAC technology.
DC11588 CC-885 CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1.
DC11578 VHL Ligand 3 A VHL ligand for PROTAC..
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