Cat. No.: HY-130612

PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect.
(Pink: BRD4 and BRD2 ligand (HY-130813); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-40178)).

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

CAS No.: 2570470-42-5
Formula: C₃₉H₃₈N₆O₉S
Molecular Weight:766.82

Storage:

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

Data Sheet (271 KB)

PROTAC BRD2/BRD4 degrader-1 Chemical Structure

CAS No.: 2570470-42-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. PROTAC BRD2/BRD4 degrader-1 effectively inhibits solid tumors with low cytotoxic effect^[1]. (Pink: BRD4 and BRD2 ligand (HY-130813); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-40178)).

IC₅₀ & Target^[1]

BRD4

BRD2

Cereblon

All Epigenetic Reader Domain Isoforms :

All PROTACs Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	GI₅₀	2.11 μM Compound: 15; LT-595-494	Growth inhibition of human 786-0 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human 786-0 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
A-375	IC₅₀	2.435 μM Compound: 15; LT-595-494	Antiproliferative activity against human A375 cells assessed as reduction in cell viability Antiproliferative activity against human A375 cells assessed as reduction in cell viability	[PMID: 31767403]
A549	GI₅₀	5.26 μM Compound: 15; LT-595-494	Growth inhibition of human A549/ATCC cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human A549/ATCC cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
A549	IC₅₀	13.74 μM Compound: 15; LT-595-494	Antiproliferative activity against human A549 cells assessed as reduction in cell viability Antiproliferative activity against human A549 cells assessed as reduction in cell viability	[PMID: 31767403]
BT-549	GI₅₀	0.078 μM Compound: 15; LT-595-494	Growth inhibition of human BT549 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human BT549 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
CAKI-1	GI₅₀	2.63 μM Compound: 15; LT-595-494	Growth inhibition of human Caki1 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human Caki1 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
CCRF-CEM	GI₅₀	0.028 μM Compound: 15; LT-595-494	Growth inhibition of human CCRF-CEM cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human CCRF-CEM cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
COLO 205	GI₅₀	0.495 μM Compound: 15; LT-595-494	Growth inhibition of human COLO205 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human COLO205 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
COLO 205	IC₅₀	0.1557 μM Compound: 15; LT-595-494	Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability Antiproliferative activity against human COLO205 cells assessed as reduction in cell viability	[PMID: 31767403]
CWR22R	IC₅₀	0.081 μM Compound: 15; LT-595-494	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability	[PMID: 31767403]
DU-145	GI₅₀	5.91 μM Compound: 15; LT-595-494	Growth inhibition of human DU145 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human DU145 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
DU-145	IC₅₀	3.66 μM Compound: 15; LT-595-494	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability Antiproliferative activity against human DU145 cells assessed as reduction in cell viability	[PMID: 31767403]
EKVX	GI₅₀	7.48 μM Compound: 15; LT-595-494	Growth inhibition of human EKVX cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human EKVX cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HCC 2998	GI₅₀	0.316 μM Compound: 15; LT-595-494	Growth inhibition of human HCC2998 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HCC2998 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HCC827	IC₅₀	0.5802 μM Compound: 15; LT-595-494	Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability Antiproliferative activity against human HCC827 cells assessed as reduction in cell viability	[PMID: 31767403]
HCT-116	GI₅₀	3.66 μM Compound: 15; LT-595-494	Growth inhibition of human HCT116 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HCT116 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HL-60(TB)	GI₅₀	0.022 μM Compound: 15; LT-595-494	Growth inhibition of human HL-60(TB) cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HL-60(TB) cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HOP-62	GI₅₀	0.416 μM Compound: 15; LT-595-494	Growth inhibition of human HOP62 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HOP62 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HOP-92	GI₅₀	0.026 μM Compound: 15; LT-595-494	Growth inhibition of human HOP92 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HOP92 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
Hs-578T	GI₅₀	0.186 μM Compound: 15; LT-595-494	Growth inhibition of human Hs 578T cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human Hs 578T cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
HT-29	GI₅₀	3.77 μM Compound: 15; LT-595-494	Growth inhibition of human HT-29 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human HT-29 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
IGROV-1	GI₅₀	0.145 μM Compound: 15; LT-595-494	Growth inhibition of human IGROV1 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human IGROV1 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
K562	GI₅₀	0.422 μM Compound: 15; LT-595-494	Growth inhibition of human K562 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human K562 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
KM12	GI₅₀	0.675 μM Compound: 15; LT-595-494	Growth inhibition of human KM12 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human KM12 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
LNCaP	IC₅₀	0.62 μM Compound: 15; LT-595-494	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability	[PMID: 31767403]
LNCaP-Clone-FGC	IC₅₀	0.9095 μM Compound: 15; LT-595-494	Antiproliferative activity against human LNCaP-FGC cells assessed as reduction in cell viability Antiproliferative activity against human LNCaP-FGC cells assessed as reduction in cell viability	[PMID: 31767403]
LOX IMVI	GI₅₀	3.97 μM Compound: 15; LT-595-494	Growth inhibition of human LOXIMVI cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human LOXIMVI cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
M14	GI₅₀	0.937 μM Compound: 15; LT-595-494	Growth inhibition of human M14 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human M14 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
Malme-3M	GI₅₀	0.161 μM Compound: 15; LT-595-494	Growth inhibition of human MALME-3M cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MALME-3M cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MCF7	GI₅₀	0.303 μM Compound: 15; LT-595-494	Growth inhibition of human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MDA-MB-231	GI₅₀	0.032 μM Compound: 15; LT-595-494	Growth inhibition of human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MDA-MB-435	GI₅₀	0.819 μM Compound: 15; LT-595-494	Growth inhibition of human MDA-MB-435 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-435 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MDA-MB-468	GI₅₀	0.02 μM Compound: 15; LT-595-494	Growth inhibition of human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MOLM-13	IC₅₀	0.05196 μM Compound: 15; LT-595-494	Antiproliferative activity against human MOLM13 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM13 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay	[PMID: 31767403]
MOLT-4	GI₅₀	0.031 μM Compound: 15; LT-595-494	Growth inhibition of human MOLT4 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human MOLT4 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
MV4-11	IC₅₀	0.00979 μM Compound: 15; LT-595-494	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability	[PMID: 31767403]
MV4-11	IC₅₀	0.01225 μM Compound: 15; LT-595-494	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay	[PMID: 31767403]
NCI-H1650	IC₅₀	1.332 μM Compound: 15; LT-595-494	Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability	[PMID: 31767403]
NCI-H1975	IC₅₀	0.4588 μM Compound: 15; LT-595-494	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability	[PMID: 31767403]
NCI-H226	GI₅₀	0.456 μM Compound: 15; LT-595-494	Growth inhibition of human NCI-H226 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human NCI-H226 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
NCI-H23	GI₅₀	37.5 μM Compound: 15; LT-595-494	Growth inhibition of human NCI-H23 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human NCI-H23 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
NCI-H322M	GI₅₀	0.355 μM Compound: 15; LT-595-494	Growth inhibition of human NCI-H322M cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human NCI-H322M cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
NCI-H358	IC₅₀	1.381 μM Compound: 15; LT-595-494	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability	[PMID: 31767403]
NCI-H522	GI₅₀	2.74 μM Compound: 15; LT-595-494	Growth inhibition of human NCI-H522 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human NCI-H522 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
OVCAR-3	GI₅₀	1.83 μM Compound: 15; LT-595-494	Growth inhibition of human OVCAR3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
OVCAR-4	GI₅₀	0.259 μM Compound: 15; LT-595-494	Growth inhibition of human OVCAR4 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR4 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
OVCAR-5	GI₅₀	2.74 μM Compound: 15; LT-595-494	Growth inhibition of human OVCAR5 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR5 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
OVCAR-8	GI₅₀	0.36 μM Compound: 15; LT-595-494	Growth inhibition of human OVCAR8 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human OVCAR8 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
PC-3	GI₅₀	0.248 μM Compound: 15; LT-595-494	Growth inhibition of human PC3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human PC3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
PC-3	IC₅₀	0.932 μM Compound: 15; LT-595-494	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability Antiproliferative activity against human PC3 cells assessed as reduction in cell viability	[PMID: 31767403]
RPMI-8226	GI₅₀	0.683 μM Compound: 15; LT-595-494	Growth inhibition of human RPMI8226 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human RPMI8226 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
RPMI-8226	IC₅₀	0.4395 μM Compound: 15; LT-595-494	Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability Antiproliferative activity against human RPMI8226 cells assessed as reduction in cell viability	[PMID: 31767403]
RXF 393	GI₅₀	0.864 μM Compound: 15; LT-595-494	Growth inhibition of human RXF393 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human RXF393 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SF-268	GI₅₀	0.366 μM Compound: 15; LT-595-494	Growth inhibition of human SF268 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SF268 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SF-295	GI₅₀	3.22 μM Compound: 15; LT-595-494	Growth inhibition of human SF295 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SF295 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SF-539	GI₅₀	0.752 μM Compound: 15; LT-595-494	Growth inhibition of human SF539 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SF539 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SK-MEL-2	GI₅₀	1.12 μM Compound: 15; LT-595-494	Growth inhibition of human SK-MEL-2 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SK-MEL-2 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SK-MEL-28	GI₅₀	0.891 μM Compound: 15; LT-595-494	Growth inhibition of human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SK-MEL-28 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SK-MEL-5	GI₅₀	1.12 μM Compound: 15; LT-595-494	Growth inhibition of human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SK-MEL-5 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SK-OV-3	GI₅₀	1.63 μM Compound: 15; LT-595-494	Growth inhibition of human SKOV3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SKOV3 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SN12C	GI₅₀	0.447 μM Compound: 15; LT-595-494	Growth inhibition of human SN12C cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SN12C cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SNB-19	GI₅₀	0.475 μM Compound: 15; LT-595-494	Growth inhibition of human SNB19 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SNB19 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SNB-75	GI₅₀	0.089 μM Compound: 15; LT-595-494	Growth inhibition of human SNB75 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SNB75 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SR	GI₅₀	0.122 μM Compound: 15; LT-595-494	Growth inhibition of human SR cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SR cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
SW-620	GI₅₀	0.249 μM Compound: 15; LT-595-494	Growth inhibition of human SW620 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human SW620 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
T47D	GI₅₀	0.034 μM Compound: 15; LT-595-494	Growth inhibition of human T47D cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human T47D cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
TK-10	GI₅₀	0.895 μM Compound: 15; LT-595-494	Growth inhibition of human TK10 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human TK10 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
TT	IC₅₀	0.0374 μM Compound: 15; LT-595-494	Antiproliferative activity against human TT cells assessed as reduction in cell viability Antiproliferative activity against human TT cells assessed as reduction in cell viability	[PMID: 31767403]
UACC-62	GI₅₀	5.45 μM Compound: 15; LT-595-494	Growth inhibition of human UACC62 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay Growth inhibition of human UACC62 cells assessed as cell growth inhibition incubated for 48 hrs by sulforhodamine B assay	[PMID: 31767403]
VCaP	IC₅₀	0.2504 μM Compound: 15; LT-595-494	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability Antiproliferative activity against human VCaP cells assessed as reduction in cell viability	[PMID: 31767403]

In Vitro

PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC₅₀ value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines^[1].
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI₅₀ values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells^[1].
PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC₅₀: 0.081 μM), colon cancer (colo-205 IC₅₀: 0.1557 μM) and thyroid cancer(TT IC₅₀: 0.037451 μM)^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MV4-11 leukemia cells
Concentration:

100 nM
Incubation Time:

≥8 hours
Result:

The BRD4 protein was reduced very efficiently.

Western Blot Analysis^[1]

Cell Line:

MV4-11 leukemia cells
Concentration:

10 , 50, 100, 500 nM
Incubation Time:

18 hours
Result:

Performed depletion selectivity for BRD4 and BRD2 over BRD3, with good selectivity intra-BET proteins selectivity.

Chemical Information

CAS No. 2570470-42-5
Molecular Weight 766.82
Formula C₃₉H₃₈N₆O₉S
SMILES

O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC4=CC5=C(NS(=O)(C6=CC=CC=C6OC)=O)C=CC(N(C)C7=O)=C5C7=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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PROTAC BRD2/BRD4 degrader-1

All Epigenetic Reader Domain Isoforms

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Biological Activity

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References

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PROTAC BRD2/BRD4 degrader-1 Related Classifications

HY-130612 Related Classifications