DC9293 |
MS023
Featured
|
MS023 is a potent, selective, and cell-active inhibitor of human type I PRMTs with IC50 of 4-119 nM. |
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DC8805 |
MS049 (hydrochloride)
Featured
|
MS049 is a potent and selective inhibitor of PRMT4 and PRMT6 that is active in cells. |
|
DC7682 |
MS417
Featured
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MS417 is a novel BrD inhibitor with high affinity and specificity For the BrDs of BET proteins. pIC50 7.52 (IC50 30 nM). |
|
DC11063 |
MS645 |
MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2. |
|
DC10023 |
MT-1
Featured
|
MT1 is a bivalent chemical probe of BET bromodomains.MT1 is an intramolecular bivalent BRD4 binder that is more than 100-fold more potent, in cellular assays, than the corresponding monovalent antagonist, JQ1. |
|
DC8823 |
XY1
Featured
|
Negative control of SGC 707. Exhibits >3000-fold lower potency (IC50 >100 μM) compared to the active analog. |
|
DC7548 |
Nexturastat A
Featured
|
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM, >190-fold selectivity over other HDACs. |
|
DC9758 |
NI-57
Featured
|
NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry. |
|
DC7850 |
OF-1
Featured
|
OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively. |
|
DC5204 |
OG-L002
Featured
|
OG-L002 is a potent and specific LSD1 inhibitor with IC50 of 20 nM, exhibiting 36- and 69-fold selectivity over MAO-B and MAO-A, respectively. |
|
DC9985 |
OICR9429
Featured
|
OICR-9429 is a potent and selective chemical probe suitable to help dissect the biological role of WDR5 (Kdisp < 100 nM). |
|
DC10658 |
OSS-128167(SIRT6-IN-1)
Featured
|
OSS-128167 is a novel SIRT6 inhibitor. |
|
DC11257 |
OTS186935
Featured
|
OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model. |
|
DC11256 |
OTS193320
Featured
|
OTS193320 (OTS-193320) is a potent inhibitor of protein methyltransferase SUV39H2 with IC50 of 22.2 nM. |
|
DC7183 |
Panobinostat(LBH589)
Featured
|
Panobinostat(LBH-589) is a broad-spectrum HDAC inhibitor; low nanomolar concentrations (IC50=5-20 nM) of LBH589 induced cell-cycle arrest, apoptosis, and histone (H3K9 and H4K8) hyperacetylation in MOLT-4 and Reh cell. |
|
DC1109 |
PCI-34051
Featured
|
PCI-34051 is a potent and specific HDAC8 inhibitor with IC50 of 10 nM. |
|
DC10634 |
PF-06726304 |
PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM. |
|
DC11153 |
PF-06855800 |
PF-06855800 (PF06855800) is a potent, selective, SAM competitive, BBB-penetrant, orally active inhibitor of protein arginine methyltransferase PRMT5 with Ki of 0.02 nM. |
|
DC9305 |
PF-CBP1(PF-06670910) hydrochloride
Featured
|
PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons. |
|
DC5025 |
PFI-1 (PF-6405761)
Featured
|
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM. |
|
DC7679 |
(R)PFI-2 HCl
Featured
|
PFI-2 is a novel potent and selective SETD7 histone lysine methyltransferase inhibitor with IC50 ~2 nM. It has > 100-fold selectivity over other methyltransferases and other non-epigenetic targets. |
|
DC7649 |
PFI-3
Featured
|
PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively. |
|
DC8291 |
PFI-4
Featured
|
PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM). |
|
DC8661 |
Pimelic Diphenylamide 106(TC-H 106)
Featured
|
Pimelic diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs. |
|
DC10786 |
PLX51107
Featured
|
PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation. |
|
DC7280 |
Pracinostat(SB939)
Featured
|
Pracinostat(SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6; has no activity against the class III isoenzyme SIRT I. |
|
DC12248 |
PROTAC BET degrader-2 |
PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins with an IC50 value of 9.6 nM in cell growth inhibition in the RS4;11 cells and capable of achieving tumor regression. |
|
DC8654 |
PTACH (NCH-51)
Featured
|
PTACH (NCH-51) is a SAHA-based novel inhibitor of human HDAC. PTACH exerts potent growth inhibition against various human cancer cells, with EC50 values ranging from 1 to 10 μM. |
|
DC11041 |
QCA276 |
QCA276 is a novel potent BET proteins inhibitor with IC50/Ki of 10/.3 nM, QCA276 is the BET ligand for PROTAC QCA570. |
|
DC7176 |
Quisinostat (JNJ-26481585) 2HCl
Featured
|
Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11. |
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