Epigenetic Reader Domain Inhibitor

GSK 4027 (Standard) is the analytical standard of GSK 4027 (HY-101027). This product is intended for research and analytical applications. GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

XD14 (Standard) is the analytical standard of XD14 (HY-110215). This product is intended for research and analytical applications. XD14 is a potent BET inhibitor with antitumor effect. It binds to BRD2, BRD3, and BRD4 with K_ds of 170, 380, and 160 nM, respectively.

BMS-986158 (Standard) is the analytical standard of BMS-986158 (HY-101567). This product is intended for research and analytical applications. BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively.

SF2523 (Standard) is the analytical standard of SF2523 (HY-101146). This product is intended for research and analytical applications. SF2523 is a highly selective and potent inhibitor of PI3K with IC50s of 34 nM, 158 nM, 9 nM, 241 nM and 280 nM for PI3Kα, PI3Kγ, DNA-PK, BRD4 and mTOR, respectively.

BRD7-IN-1 (Standard) is the analytical standard of BRD7-IN-1 (HY-111905). This product is intended for research and analytical applications. BRD7-IN-1, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).

Ziftomenib (Standard) is the analytical standard of Ziftomenib (HY-132001). This product is intended for research and analytical applications. Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

NSC 228155 (Standard) is the analytical standard of NSC 228155 (HY-101084). This product is intended for research and analytical applications. NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM.

Birabresib (Standard) is the analytical standard of Birabresib. This product is intended for research and analytical applications. Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC₅₀s ranging from 92 to 112 nM.

ZEN-3219 (Standard) is the analytical standard of ZEN-3219 (HY-111977). This product is intended for research and analytical applications. ZEN-3219 is a BET inhibitor with IC₅₀s of 0.48, 0.16 and 0.47 μM for BRD4(BD1), BRD4(BD2) and BRD4(BD1BD2), respectively. ZEN-3219 can be used to form PROTACs to induce degradation of BRD4.

Vadenersen is an inhibitor of MECP2 protein expression. Vadenersen has potential for research into Rett syndrome.

(±)-JQ1 is the racemate of (+)-JQ-1 (HY-13030).

BRD4 Inhibitor-33 (example 13) is a BRD4 inhibitor that can be used in acute kidney disease and chronic kidney disease research.

I-BET762 carboxylic acid (Standard) is the analytical standard of I-BET762 carboxylic acid (HY-107443). This product is intended for research and analytical applications. I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC₅₀ of 5.1.

NI-42 (Standard) is the analytical standard of NI-42 (HY-101121). This product is intended for research and analytical applications. NI-42 (compound 13-d), a structurally orthogonal chemical probe for the BRPFs, is a biased, potent inhibitor of the BRD of the BRPFs (IC50s of BRPF1/2/3=7.9/48/260 nM; Kds of BRPF1/2/3=40/210/940 nM) with excellent selectivity over nonclass IV BRD proteins.

Mivebresib (Standard) is the analytical standard of Mivebresib. This product is intended for research and analytical applications. Mivebresib (ABBV-075) is a potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.

CPI-637 (Standard) is the analytical standard of CPI-637 (HY-100482). This product is intended for research and analytical applications. CPI-637 is a selective and potent CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM, 0.051 μM and 11.0 μM for CBP, EP300 and BRD4 BD-1, respectively, and an EC50 of 0.3 μM for CBP.

IACS-9571 hydrochloride (Standard) is the analytical standard of IACS-9571 hydrochloride (HY-102000B). This product is intended for research and analytical applications. IACS-9571 (ASIS-P040) hydrochloride is a potent and selective inhibitor of TRIM24 and BRPF1, with an IC₅₀ of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

PLX51107 (Standard) is the analytical standard of PLX51107 (HY-111422). This product is intended for research and analytical applications. PLX51107 is a potent and selective BET inhibitor, with K_ds of 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1, and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively; PLX51107 also interacts with the bromodomains of CBP and EP300 (K_d, in the 100 nM range).

Menin-MLL-IN-35 (compound 286) is an inhibitor of menin/MLL protein/protein interaction with an IC₅₀ value of 0.096 μM in MEIS1 mRNA expression. Menin-MLL-IN-35 can be used in the research of cancer, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), and diabetes.

BI 2536 (Standard) is the analytical standard of BI 2536 (HY-50698). This product is intended for research and analytical applications. BI 2536 is a dual PLK1 and BRD4 inhibitor with IC₅₀s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.