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Isoforms Recommended:	NSD2/MMSET/WHSC1

Results for "

NSD2

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (2) E3 Ligase Ligand-Linker Conjugates (1) Histone Methyltransferase (17) Phosphatase (1) PROTACs (2) Small Interfering RNA (siRNA) (1)
By Research Areas:	Cancer (21)
Oligonucleotides:	Pre-designed siRNA Sets (1) siRNAs (1)

Inhibitors & Agonists

Oligonucleotides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-161575

NSD2 ligand 1	Histone Methyltransferase	Cancer
NSD2 ligand 1 is a *NSD2* ligand. NSD2 ligand 1 can be used for synthesis of LLC0424 (HY-161574) (a PROTAC NSD2 degrader) .

HY-161574

LLC0424	PROTACs Histone Methyltransferase	Cancer
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)) .

HY-151101

MS159	PROTACs	Cancer
MS159 is a potent nuclear receptor binding SET structural domain protein 2 (NSD2) PROTACdegrader. MS159 inhibits the growth of tumour cells. MS159 is a useful chemical tool for exploring the role of NSD2 in health and disease .

HY-157251

UNC8153 TFA	Histone Methyltransferase	Cancer
UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein and the *H3K36me2* chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-138283

MR837 1 Publications Verification	Histone Methyltransferase	Cancer
MR837 is an inhibitor of *NSD2-PWWP1*. MR837 can bind with human nuclear receptor binding SET domain protein 2 (PWWP domain) .

HY-RS09588

NSD2 Human Pre-designed siRNA Set A	Small Interfering RNA (siRNA)	Others
NSD2 Human Pre-designed siRNA Set A contains three designed siRNAs for NSD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

NSD2 Human Pre-designed siRNA Set A NSD2 Human Pre-designed siRNA Set A

HY-147914

NSD2-IN-1	Apoptosis	Cancer
NSD2-IN-1 (compound 38) is a potent and high selective *NSD2-PWWP1* (nuclear receptor-binding SET domain 2-PWWP1) inhibitor, with an IC₅₀ of 0.11 μM. NSD2-IN-1 can bind to NSD2-PWWP1 and then affect the expression of genes regulated by NSD2. NSD2-IN-1 induces apoptosis and cell cycle arrest .

HY-155818

NSD2-IN-4	Histone Methyltransferase	Cancer
NSD2-IN-4 is a potent and selective *NSD2-SET* inhibitor. NSD2-IN-4 has the potential for NSD2-related diseases .

HY-161670

NSD2-PWWP1 ligand 1	Histone Methyltransferase	Cancer
NSD2-PWWP1 ligand 1 (compound 34) is a small molecule ligand targeting the NSD2-PWWP1 domain (pIC50: 8.2). NSD2 is a large multidomain protein with histone writer and histone reader functions. Dysregulation of the levels of histone methyltransferase nuclear receptor binding SET domain 2 (NSD2) may lead to a variety of hematological and solid malignancies. NSD2-PWWP1 ligand 1 binds to NSD2, reducing its enzymatic activity and inhibiting tumorigenesis .

HY-157251A

UNC8153	Histone Methyltransferase	Cancer
UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein and the *H3K36me2* chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-161796

UNC8732	Others	Cancer
UNC8732 is a *NSD2* inhibitor and degrader .

HY-155817

UNC7096	Histone Methyltransferase	Others
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 (K_d=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 .

HY-145103

UNC6934	Histone Methyltransferase	Cancer
UNC6934, a chemical probe targeting the PWWP domain, alters *NSD2* nucleolar localization.

HY-114340

LEM-14	Histone Methyltransferase	Cancer
LEM-14 is a potent *NSD2* inhibitor with an IC₅₀ of 132 µM. LEM-14 has the potential for the research of multiple myeloma .

HY-124699

MMSET-IN-1	Others	Cancer
MMSET-IN-1 is a multiple myeloma SET domain (MMSET, aka NSD2/WHSC1) inhibitor against SETD2 and MMSET with IC₅₀s of 0.49 and 3.3 μM, respectively. MMSET-IN-1 has a K_d of 1.6 μM for MMSET .

HY-15647

BRD9539 1 Publications Verification	Histone Methyltransferase	Cancer
BRD9539 is a histone methyltransferase G9a inhibitor with an IC₅₀ of 6.3 μM. BRD9539 also inhibits *PRC2* activity and is inactive against SUV39H1, NSD2 and DNMT1 .

HY-114208A

BI-9321 trihydrochloride	Histone Methyltransferase	Cancer
BI-9321 trihydrochloride is a potent, selective and cellular active *nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain* antagonist with a K_d value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells .

HY-114208

BI-9321	Histone Methyltransferase	Cancer
BI-9321 is a potent, selective and cellular active *nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain* antagonist with a K_d value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells .

HY-125244

LEM-14-1189	Histone Methyltransferase	Cancer
LEM-14-1189, a LEM-14 (HY-114340) derivative, is a *NSDs inhibitor with IC₅₀s of 418 μM (NSD1),* 111 μM (NSD2), and 60 μM (NSD3), respectively. The NSDs, histone lysine methyltransferases (HMTases), are oncoproteins, drivers of a number of tumors. LEM-14-1189 can be used for multiple myeloma (MM) research .

HY-162308

NSD-IN-3	Histone Methyltransferase Apoptosis	Cancer
NSD-IN-3 (compound 3) is a potent nuclear receptor binding SET domain (NSD) inhibitor. NSD-IN-3 inhibits NSD2-SET and NSD3-SET with IC₅₀ values of 0.81 μM and 0.84 μM, respectively. NSD-IN-3 inhibits histone H3K36 dimethylation and decreases the expression of NSDs-targeted genes in non-small cell lung cancer cells. NSD-IN-3 induces s-phase cell cycle arrest and apoptosis .

HY-168035

W4275	Histone Methyltransferase	Cancer
W4275 (Compound 42) is a selective *NSD2* inhibitor with oral activity, showing an IC₅₀ value of 17 nM. W4275 exhibits antiproliferative activity with an IC₅₀ of 230 nM against RS411 cells and significantly inhibits tumor growth in the RS411 tumor xenograft model. Pharmacokinetic analysis in mice demonstrates that W4275 has good oral bioavailability (F of 27.34%). W4275 holds promise for use in cancer research .

HY-100034

NSC 663284 3 Publications Verification DA-3003-1	Phosphatase Histone Methyltransferase	Cancer
NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC₅₀ for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively . NSC 663284 inhibits *NSD2* (IC₅₀ of 170 nM) through a direct interaction with the catalytic SET domain (K_d of 370 nM) ^[2].

HY-161576

Thalidomide-Pip-N-boc	E3 Ligase Ligand-Linker Conjugates	Cancer
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) .

NSD2 Human Pre-designed siRNA Set A		siRNAs Pre-designed siRNA Sets
NSD2 Human Pre-designed siRNA Set A contains three designed siRNAs for NSD2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

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