Epigenetic Reader Domain
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB11881 | ZXH-3-26 | 2243076-67-5 | ZXH-3-26 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), shows activity exclusively on the BRD4 BD1 (DC50/5h=5 nM) and spares degradation of BRD2 or BRD3 in cellular degradation assays; ZXH-3-26 represents the first small molecule to allow pharmacologic targeting of BRD4 without significant inhibition or degradation of BRD2 and BRD3. |
| FB12878 | ZL0420 | 2229039-45-4 | ZL0420 selectively inhibits BRD4 BD1 (IC50 = 27 nM) and BRD4 BD2 (IC50 = 32 nM). |
| FB15297 | YF-2 | 1311423-89-8 | YF-2 is a highly selective and blood-brain-barrier permeable histone acetyltransferase activator, it acetylates H3 in the hippocampus. |
| FB10843 | UNC 926 | 1184136-10-4 | UNC 926 HCl binds to MBT domain of L3MBTL protein (Kd = 3.9 µM) and block the interaction with methylated lysine on histone 4, H4K20. |
| FB12097 | Target Protein-binding Moiety 6 | 2097512-23-5 | PROTAC BRD9-binding moiety 1 is a I-BRD9-based warhead ligand for conjugation reactions of PROTAC targeting on BRD9. |
| FB11371 | BETd-260 | 2093388-62-4 | PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line. |
| FB12076 | PRI-724 | 1422253-38-0 | PRI-724 is a selective inhibitor of the CBP/β-catenin interaction. |
| FB11514 | PLX51107 | 1627929-55-8 | PLX51107 is a potent and selective BRD4 inhibitor or BET inhibitor with novel in vitro and in vivo pharmacologic properties that emulates or exceeds the efficacy of BCR signaling agents in preclinical models of CLL. |
| FB11324 | NI-57 | 1883548-89-7 | NI-57 is an orally active pan-BRPF chemical probe of the bromodomain (BRD) of the BRPFs. |
| FB16905 | NI 42 | 1884640-99-6 | NI 42 is a selective inhibitor of BRPF with Kd values of 40, 210 and 943 nM for BRPF1B, 2 and 3, respectively. It also exhibits modest activity at BRD9 (Kd = 1130 nM). |
| FB16905 | NI 42 | 1884640-99-6 | NI 42 is a selective inhibitor of BRPF with Kd values of 40, 210 and 943 nM for BRPF1B, 2 and 3, respectively. It also exhibits modest activity at BRD9 (Kd = 1130 nM). |
| FB11744 | MZP-55 | 2010159-48-3 | MZP-55 is a VHL-based PROTAC targeting on BET with pDC50/Dmax (%) values of 8.1/95, 7.5/93, 7.7/92, −/26 for Brd4 short, Brd4 long, Brd3 and Brd2 in HeLa cells, consist of I-BET726 as a warhead ligand linked to VHL ligand VH032. |
| FB11743 | MZP-54 | 2010159-47-2 | MZP-54 is a PROTAC targeting on BET, consist of a warhead I-BET726 (BET bromodomain inhibitor) linked to a VHL ligand VH032. |
| FB00635 | MS436 | 1395084-25-9 | MS436, a diazobenzene-based small compound, is an inhibitor of BRD4 bromodomains with Ki values of 30-50 nM. |
| FB09909 | Mivebresib | 1445993-26-9 | Mivebresib, also known as ABBV-075, is an inhibitor of bormodomain and extra terminal domain (BET). The Ki values of BRD2, BRD4, BRDT are 1 nM - 2.2 nM. |
| FB11750 | L-45 | 2079885-05-3 | L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM. |
| FB04098 | KG-501 | 18228-17-6 | KG-501 is histochemical substrate of alkaline phosphatases and can inhibit CREB-CBP interaction. |
| FB12682 | INCB-057643 | 1820889-23-3 | INCB057643 is an inhibitor of BET and it can reduce homologous recombination efficiency and augment PARP inhibitor activity in ovarian cancer. |
| FB10261 | GSK6853 | 1910124-24-1 | GSK6853 selectively inhibits the BRPF1 bromodomain with the pKd value of 9.5. |
| FB02686 | GSK525768A | 1260530-25-3 | GSK525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4) and has NO activity towards BET. |
| FB12021 | GSK1379725A | 1802251-00-8 | GSK1379725A is an inhibitor of Brd4 and a selective BPTF ligand (Kd=2.8 μM). |
| FB10928 | GNE-272 | 1936428-93-1 | GNE-272 is a potent and selective in Vivo Probe for the Bromodomains of CBP/EP300 (CBP IC50 = 0.02 μM, EP300 IC50 = 0.03 μM, BRET IC50 = 0.41 μM, BRD4(1) C50 = 13 μM). |
| FB11580 | FL-411 | 2118944-88-8 | FL-411 selectively inhibits BRD4 with an IC50 of 0.43 ± 0.09 μM. |
| FB11078 | EML631 | 2101206-36-2 | EML631 interacts with the Tudor-domain-containing protein Spindlin1 (SPIN1), blocking its ability to 'read' H3K4me3 marks and inhibit its transcriptional-coactivator activity. |
| FB10086 | EED226 | 2083627-02-3 | EED226 is a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED. |
| FB11875 | dBET 6 | 1950634-92-0 | dBET6 is an optimized and highly cell-permeable chemical degrader of BET bromodomain proteins, based on PROTAC. |
| FB11920 | dBET57 | 1883863-52-2 | dBET57 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=500 nM), but is inactive on BRD4 BD2. |
| FB11921 | dBET23 | 1957234-83-1 | dBET23 is a BRD4 heterobifunctional small-molecule ligand (PROTAC), exhibits significant and selective degradation of BRD4 BD1 (DC50/5h=50 nM) in cellular degradation assays. |
| FB10380 | CPI-637 | 1884712-47-3 | CPI-637 is an efficient inhibitor of CBP/EP300 bromodomain with IC50 of 0.03 ± 0.01μM. |
| FB16218 | CPI-268456 | 1380087-86-4 | CPI-268456 is a ligand of BRD4. |
| FB02816 | CPI-0610 | 1380087-89-7 | CPI-0610 is an inhibitor of BET bromodomains BRD2, BRD3, BRD4, and BRDT via binding to the acetylated lysine recognition motifs. |
| FB10870 | CD161 | 1627716-22-6 | CD161 is a potent, selective, and orally active BET inhibitor. |
| FB18249 | CBP/EP300-IN-1 | 2443789-32-8 | CBP/EP300-IN-1 is a CBP/EP300 bromodomain inhibitor. |
| FB10260 | BI-9564 | 1883429-22-8 | BI-9564 is an inhibitor of BRD9 (IC50 = 75 nM) and BRD7 (IC50 = 3.4 µM). |
| FB02581 | BI-7273 | 1883429-21-7 | BI-7273 is a potent, selective, and cell-permeable BRD9 BD Inhibitor. |
| FB11923 | BETd-246 | 2140289-17-2 | BETd-246 is a second-generation BET bromodomain inhibitor. It causes a dose-dependent depletion of BRD2, BRD3 and BRD4 in representative TNBC cell lines with 30-100 nM for 1 h or with 10-30 nM for 3 h incubation. |
| FB03198 | BET-IN-1 | 1422554-34-4 | BET-IN-1 is a bromodomain inhibitor with a plC50 in the range 6.0 - 7.0. |
| FB10265 | BET-BAY 002 S-Enantiomer | 2070009-49-1 | BET-BAY 002 S-enantiomer is the S-enantiomer of BET-BAY 002. |
| FB03308 | BET-BAY 002 | 1588521-78-1 | BET-BAY 002 is a potent BET inhibitor and shows efficacy in a multiple myeloma model. |
| FB11190 | BET Inhibitor C3 | 874594-37-3 | BET inhibitor C3 is a BET bromodomain inhibitor of epigenetic regulatory proteins BrdT and Brd4. |
| FB11279 | AZD5153 6-Hydroxy-2-Naphthoic Acid | 1869912-40-2 | AZD5153 is an inhibitor of BET/BRD4 bromodomain, the IC50 for BRD4 is 1.7 nM. |
| FB09899 | AZD5153 | 1869912-39-9 | AZD5153 exhibits excellent pharmacokinetic profile and high potency in vitro and in vivo effecting c-Myc downregulation and tumor growth inhibition in xenograft studies. |
| FB11768 | AT6 | 2098836-50-9 | AT6 is a PROTAC targeting on Brd4. |
| FB11767 | AT 1 | 2098836-45-2 | AT1 is a highly selective Brd4 degrader with a modified VHL ligand retained binding to VHL (Kd = 330 nM). |
| FB04023 | ARV-825 | 1818885-28-7 | ARV-825 is a PROTAC targeting on BRD4, consisting of a BRD4-ligand JQ-1 linked to a cereblon E3 ligase ligand Pomalidomide, with Kds values of 90nM and 28nM for affinity to BD1 and BD2. |
| FB11647 | EED inhibitor-1 | 1951408-58-4 | An inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity. |
| FB17248 | Alobresib | 1637771-14-2 | Alobresib is a BET bromodomain inhibitor, a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. |
| FB11595 | ABBV-744 | 2138861-99-9 | ABBV-744 is an inhibitor of BDII-selective BET bromodomain that is being investigated to treat AML and metastic castration-resistant prostate cancer. |
| FB15614 | 666-15 | 1433286-70-4 | 666-15 is a potent and cell-permeable inhibitor of cAMP-response element binding protein (CREB) with efficacious anti-cancer activity both in vitro and in vivo. |
| FB04062 | JQ-1 Carboxylic Acid | 202592-23-2 | (+)-JQ1 carboxylic acid is a warhead ligand with a carboxylic acid functional group for conjugation reactions of PROTAC targeting on BET. |