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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
14 Results for "
H3K36me2
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "H3K36me2" in MCE Product Catalog:
1
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Gintemetostat (KTX-1001) is an orally active, highly specific NSD2/MMSET histone methyltransferase inhibitor with human NSD2 IC50 values ranging 0.460-2.17 nM and NSD2 SET domain IC50 of 2.32 nM and Kd values ranging 6.3-70.4 nM .Gintemetostat reduces H3K36me2 levels, impairs multiple myeloma cell adhesion and colony formation, enhances cytotoxicity, boosts T-cell activation, and sensitizes resistant multiple myeloma cells to other agents .Gintemetostat can be used for the research of multiple myeloma and relapsed and refractory multiple myeloma .
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UNC6934 is a selective NSD2-PWWP1 antagonist with a Kd of 91 nM against human targets. UNC6934 binds to the canonical methyl-lysine binding pocket of NSD2-PWWP1 and directly competes with H3K36me2 for binding. UNC6934 induces the aggregation of NSD2 within the nucleolus, without altering ribosomal RNA transcription, global H3K36me2 levels or the proliferation of KMS-11 cells. UNC6934 can be used in studies related to multiple myeloma and diffuse intrinsic pontine glioma .
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UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
Cat. No.: HY-179427
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NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC) .
Cat. No.: HY-161574
CAS No.: 3061315-33-8
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LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
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UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a Kd of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC50 in cell U2OS is 0.35 μM) and the H3K36me2 chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .
Cat. No.: HY-155817
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UNC7096 (compound 53) is a biotinylated affinity reagent. The phenyl ring of UNC7096 replaces the pyrimidine ring in UNC6934 (HY-145103) and introduces biotin at the para position of the phenyl ring, which has a high binding affinity to the NSD2-PWWP1 domain (Kd=46 nM). UNC7096 blocks the interaction between NSD2-PWWP1 and nucleosomal H3K36me2 by occupying the methyl-lysine binding pocket of NSD2-PWWP1. This binding is achieved by covalent binding through the formation of hydrogen bonds and a specific aromatic cage structure. UNC7096 can be used to capture proteins that interact with the NSD2-PWWP1 domain to further analyze the biological significance of these interactions .
Cat. No.: HY-161796
CAS No.: 2929304-05-0
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UNC8732 is an NSD2 degrader with a Kd value of 76 nM for NSD2, and achieves highly selective degradation of NSD2 across the detectable proteome. UNC8732 acts as a prodrug; its primary amine is metabolized to an aldehyde, which forms a reversible covalent interaction with Cys326 in the FIST_C domain of FBXO22, recruiting the SCFFBXO22 ubiquitin ligase complex to mediate polyubiquitination and proteasomal degradation of NSD2. UNC8732 serves as a chemical probe to investigate NSD2-associated disease phenotypes and study the functions of NSD2 in nuclear signaling and epigenetics. UNC8732 can be used in studies of acute lymphoblastic leukemia .
Cat. No.: HY-180553
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NSD2-IN-6 is a selective and orally active NSD2 inhibitor with IC50s of 3.8 and 274 nM for NSD2 and NSD1 respectively. NSD2-IN-6 reduces H3K36me2 levels, reverses cell plasticity by restoring the androgen receptor ( AR) signaling pathway. NSD2-IN-6 reduces a shift from cluster 2 and 3 states towards the cluster 1 state in organoids. NSD2-IN-6 exerts antitumor activity by reversing tumor cell plasticity, suppressing growth, and promoting apoptosis in vivo. NSD2-IN-6 can be used for prostate cancer research .
Cat. No.: HY-187178
CAS No.: 1966932-74-0
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KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC50 of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers .
Cat. No.: HY-179651
CAS No.: 106664-01-1
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NSD2-PWWP1-IN-6 (Compound 16) is an effective NSD2-PWWP1 inhibitor with a Kd value of 30 nM. NSD2-PWWP1-IN-6 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-6 can be used for cancer research .
Cat. No.: HY-179650
CAS No.: 217798-45-3
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NSD2-PWWP1-IN-5 (Compound 13) is an effective NSD2-PWWP1 inhibitor with a Kd value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma .
Cat. No.: HY-161576
CAS No.: 2636798-54-2
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Thalidomide-Pip-N-boc is a conjugate of E3 ligase ligand and linker. Thalidomide-Pip-N-boc is utilized for synthesis of PROTAC Degrader LLC0424 (HY-161574) .
Cat. No.: HY-185557
CAS No.: 3063448-59-6
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LLC0424N is a negative control compound designed by methylating the thalidomide moiety of LLC0424 (HY-161574). LLC0424N shows does not induce NSD2 degradation and inhibit growth of acute lymphoblastic leukemia cells with NSD2 mutation. LLC0424N can be used for the research of acute lymphoblastic leukemia .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
