PROTAC BRD2/BRD4 degrader-1

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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. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.

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PROTAC BRD2/BRD4 degrader-1 Chemical Structure

CAS No. : 2570470-42-5

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•Related Small Molecules:

•Related Proteins:

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BRD4

BRD2

Cereblon

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]
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]
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]
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]
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]
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]
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.

Molecular Weight

766.82

Formula

C₃₉H₃₈N₆O₉S

CAS No.

2570470-42-5

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

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]