IKZF Family Inhibitor

NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the D_max and DC₅₀ of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC₅₀: 13 nM) and SALL4 (DC₅₀: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2.

ALV1 is a molecular glue degrader for Ikaros (IKZF1) and Helios (IKZF2) with DC₅₀ of 2.5 nM and 10.3 nM respectively. ALV1 bind CRBN with an IC₅₀ of 0.55 μM, and induces CRBN-Helios dimerization. ALV1 can be used to study the properties and functions of regulatory T cells.

(R)-BMS-986449 is the racemic mixture of BMS-986449 (HY-173630). BMS-986449 is a CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors.

BMS-986449 is a potent and orally active CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors.

GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC₅₀ of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.

KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC₅₀ values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma.

SZU305 is a RAD51 PROTAC degrader, with DC₅₀ values of 307.45 nM and 84.19 nM in SK-HEP-1 and Huh-7 cells, respectively. SZU305 inhibits DNA damage repair, induces cell cycle arrest and apoptosis. SZU305 moderately reduces the protein levels of IKZF1 and IKZF3 at high concentrations. SZU305 can be used in studies related to hepatocellular carcinoma.

GATA4-NKX2-5-IN-1 (Standard) is the analytical standard of GATA4-NKX2-5-IN-1 (HY-103484). This product is intended for research and analytical applications. GATA4-NKX2-5-IN-1 (Compound 3) dose-dependently inhibits the GATA4–NKX2-5 transcriptional synergy with an IC₅₀ of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.