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CC-885

  Cat. No.:  DC11588   Featured
Chemical Structure
1010100-07-8
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More than 5000 active chemicals with high quality for research!
Field of application
CC-885 (CC 885, CC885) is a novel E3 ligase cereblon (CRBN) modulator with potent anti-tumour activity mediated through the degradation of GSPT1.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1010100-07-8
Chemical Name: CC-885
Synonyms: CC-885;N-(3-chloro-4-methylphenyl)-N'-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1-oxo-1H-isoindol-5-yl]methyl]-urea;1-(3-chloro-4-methylphenyl)-3-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)methyl)urea;1-(3-chloro-4-methylphenyl)-3-[[2-(2,6-dioxopiperidin-3-yl)-1-oxo-3H-isoindol-5-yl]methyl]urea;GTPL9224;TQR1238;s8300;J3.571.763C;1-(3-Chloro-4-methyl-phenyl)-3-[2-(2,6-dioxo-piperidin-3-yl)-1-oxo-2,3-dihydr
SMILES: ClC1=C(C)C=CC(=C1)NC(NCC1C=CC2C(N(CC=2C=1)C1C(NC(CC1)=O)=O)=O)=O
Formula: C22H21ClN4O4
M.Wt: 440.879544019699
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity.
Target: CRBN[1].
In Vitro: Acute myeloblatlic leukemia (AML) cell lines, human liver epithelial cell line (THLE-2) and human peripheral blood mononuclear cells (PBMC) are treated with varying concentrations of CC-885, with IC50s of 10×-6-1 μM. The effect of CC-885 on cell proliferation in AML cell lines, THLE-2 and human PBMC is more powerful than Lenalidomide and Pomalidomide with IC50s>10 μM. To address whether the cereblon-dependent degradation of GSPT1 is responsible for the cytotoxic effects of CC-885, a GSPT1 mutant that retains its normal function, but loses CC-885-dependent cereblon binding, is used to distinguish the role of GSPT1 from that of other substrates. CC-885 is tested in 293T HEK cells stably expressing the CC-885-sensitive or -resistant GSPT1 variants. Overexpression of a resistant variant GSPT1Δ(1–138)/(G575N) completely abrogate the CC-885-induced anti-proliferation, whereas overexpression of a CC-885-sensitive variant GSPT1Δ(1-138) only confer partial protection. Similar results are obtained in AML cell lines[1].
Cell Assay: Human cancer cell lines cultured in the growth medium are seeded into black 384-well plates containing DMSO or test compounds such as CC-885 (10×-6-1 μM). The seeding density for each cell line is optimized to allow the cell growth in the linear range during a 3-day culture period. To test the compound effect on cell proliferation in acute myeloid leukaemia (AML) cell lines, 5,000 to 10,000 cells per well in 200 μl complete culture media are seeded into black 96-well plates containing DMSO or test compounds such as CC-885. After 48 or 72 h, cell proliferation is assessed using the CellTiter-Glo (CTG) Luminescent Cell Viability Assay[1].
References: [1]. Mary E. Matyskiela, et al. A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase. Nature. 2016 Jul 14;535(7611):252-7.
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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