Epigenetic Reader Domain Inhibitor

Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding K_i of 0.149 nM and a cell based IC₅₀ of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).

5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.

666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

MZ 1 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4. MZ 1 potently and rapidly induces reversible, long-lasting, and selective removal of BRD4 over BRD2 and BRD3. K_ds of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively.

VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 has potently anti-leukemia activity.

I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC₅₀ of 6.1, 6.3, and 6.6, respectively.

Ziftomenib (KO-539) is an orally active menin-MLL interaction inhibitor with antitumor activities (WO2017161028A1, compound 151).

KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC₅₀ of 32.5-42.5 nM.

GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC₅₀ of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC₅₀s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model.

ATF3 inducer 1 is a potent ATF3 inducer. ATF3 inducer 1 increases the ATF3 protein and ATF3 mRNA expression. ATF3 inducer 1 shows anti-MetS activity in mouse.

Apabetalone (RVX-208) is an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. The IC₅₀s are 87 μM and 0.51 μM for BD1 and BD2, respectively.

BAY-850, a chemical probe, is a potent and isoform selective ATPase family AAA domain-containing protein 2 (ATAD2) inhibitor, with an IC₅₀ of 166 nM.

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC₅₀ of value of 5 nM for full-length BRD4 (FL-BRD4). AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 can be used for the study of cancer, such as acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma.

I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC₅₀ value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways.

PKI 14-22 amide, myristoylated is a selective, cAMP-dependent, competitive PKA inhibitor with K_i=~36 nM. The myristoylation modification of PKI 14-22 amide, myristoylated makes it more permeable to cell membranes and blood-brain barriers than the precursor molecule. PKI 14-22 amide, myristoylated can block the phosphorylation of cAMP-dependent downstream targets (such as CREB). PKI 14-22 amide, myristoylated can prevent the development of morphine analgesic tolerance in mice, and also inhibits protein translation and negative-strand RNA synthesis of Zika virus. PKI 14-22 amide, myristoylated can be used in research fields such as opioid tolerance mechanisms and antiviral drugs.

dTRIM24 is a selective bifunctional degrader of TRIM24 based on PROTAC, consists of ligands for von Hippel-Lindau and TRIM24.

Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.

Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes.