1. Epigenetics PROTAC
  2. Histone Acetyltransferase Epigenetic Reader Domain PROTACs
  3. BT-O2C

BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC::DUX4 sarcoma (CDS) cell lines (IC50 = 152-221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer.(Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).

For research use only. We do not sell to patients.

BT-O2C Chemical Structure

BT-O2C Chemical Structure

CAS No. : 3055107-34-8

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Description

BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC::DUX4 sarcoma (CDS) cell lines (IC50 = 152-221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer.(Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869))[1].

IC50 & Target[1]

p300

 

Cereblon

 

In Vitro

BT-O2C (0.1-10 μM, 24 h) can significantly degrade p300 and has almost no effect on the degradation of CBP in HAPI cells[1].
BT-O2C (0.25-4 μM, 48-72 h) exhibits significant cytotoxicity in NCC-CDS1-X1 (IC50 = 152 nM) and KITRA (IC50 = 221 nM) cells[1].
BT-O2C (4 μM, 6 h) significantly reduces the expression of CDS target genes in NCC-CDS-X1 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HAPI cells
Concentration: 0.1, 1 and 10 μM
Incubation Time: 24 h
Result: Selectively degraded the protein level of p300, superior to JQAD1 (HY-145765).

RT-PCR[1]

Cell Line: NCC-CDS-X1 cells
Concentration: 4 μM
Incubation Time: 6 h
Result: Significantly reduced the expression of ETV1, ETV4, ETV5, CCNEE1 and MYC.
Molecular Weight

973.94

Formula

C48H48F5N9O8

CAS No.
SMILES

O=C(N(CC1=CC=C(F)C=C1)[C@@H](C)C(F)(F)F)CN(C(N[C@]23C[C@@H](F)C4=C3C=CC(C5=CN(CC(NCCCCCCCNC6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)=O)N=C5)=C4)=O)C2=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BT-O2C
Cat. No.:
HY-174866
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