|Description||CPI-0610, a benzazepine derivative, has been found to influence tumor cell growth at some extent by acting as a BET bromodomain inhibitor. IC50: < 500 nM for BRD4. It is still under a Phase I trial for Leukaemia, Lymphoma and sorts of other cancers.|
|Solubility||10 mM in DMSO|
|Application||CPI-0610 has been found to influence tumor cell growth at some extent by acting as a BET bromodomain inhibitor.|
|Shelf Life||As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly|
|Current Developer||Constellation Pharmaceuticals; The Leukemia & Lymphoma Society|
XD 14 is a BET bromodomain inhibitor (Kd = 160, 170, 380, 490, 830 and 850 nM for BRD4(1), BRD2(1), BRD3(1), BRD3(2), BRD2(2) and BRD4(2) respectively). XD 14 a...
I-BET 151 dihydrochloride
The hydrochloride salt form of I-BET 151, which has been found to be a BET bromodomain inhibitor and exhibit activities against human and murine MLL-fusion leuk...
ISOX INACT is an inactive control probe of the bromodomain of CREB binding protein (CBP) PF-CBP1. It shows negligible activity at CBP and BRD4. It was used to p...
OTX015 a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD). BRDs 2, 3, and 4 are considered potential cancer target...
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor with IC50 of 80 nM.
MS436 exhibits low nanomolar affinity with preference for the first bromodomain over the second.
CPI-0610, a benzazepine derivative, has been found to influence tumor cell growth at some extent by acting as a BET bromodomain inhibitor. IC50: < 500 nM for BR...
TPOP146 is a potent and selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4. TPOP146 targets the CBP br...
AZD5153 6-Hydroxy-2-naphthoic acid
AZD5153 6-Hydroxy-2-naphthoic acid, a 6-hydroxy-2-naphthoic acid salt of AZD-5153, is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor p...
Mivebresib is a BET inhibitor with potential antineoplastic activity. It disrupts critical transcription programs that drive prostate cancer growth to induce po...
Olinone, a pyridoindol derivative, has been found to be an BET Bromodomain inhibitor and could be probably useful in sorts of biological studies.
LP99 is the first selective BRD7/9 bromodomain inhibitor. The effect of LP99 on IL-6 expression demonstrates for the first time that a small-molecule BRD7/9 in...
BET bromodomain inhibitor
An BET bromodomain inhibitor can be used for the treatment of hematologic malignancies. It binds BET proteins to suppress the interaction between these proteins...
BET-BAY 002 is a potent BET inhibitor with strong in vitro and in vivo activities in AML and MM models, and with excellent pharmacokinetic properties.
BI-2563 is a small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arr...
I-BET151, also known as GSK1210151A, is a BET bromodomain inhibitor, which blocks recruitment of BET to chromatin. I-BET151 (GSK1210151A) shows good oral bioava...
OXF BD 02
OXF BD 02 is a first bromodomain of BRD4 inhibitor with IC50 value of 382 nM. It can reduce viability of lung adenocarcinoma cell lines and attenuate proliferat...
The (R) - isomer form of JQ1 which is a BET inhibitor that could probably influence the inflammatory expression at some extent.
PF-CBP1, also known as PF-06670910, is a selective CBP/p300 bromodomain inhibitor (IC50 values are 125 and 363 nM, respectively) with >100-fold selectivity for ...
GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), ...