2. Epigenetics
  3. Histone Methyltransferase
  4. NSD2-IN-6

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.

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NSD2-IN-6

NSD2-IN-6 Chemical Structure

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Other Forms of NSD2-IN-6:

NSD2-IN-6 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

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[1].

IC50 & Target[1]

EZH1

3.8 nM (IC50)

EZH1

274 nM (IC50)

In Vitro

NSD2-IN-6 (compound NSD2i) shows a substantial reduction in H3K36me2 domains in NPPO-1NE organoids[1].
NSD2-IN-6 results a substantial shift from cluster 2 and 3 states towards the cluster 1 state and enrichment of canonical AR target expression in NPPO-1NE organoids[1].
NSD2-IN-6 has little or no effect on AR expression in non-neuroendocrine organoids with combined Enzalutamide [1].
NSD2-IN-6 (1 µM, 17 days) increases sensitivity to enzalutamide in NPPO-1NE, NPPO-2, NPPO-4 and NPPO-6 organoids with EC50 values of 0.34, 2.7, 1.6 and 20 µM respectively[1].
NSD2-IN-6 (0.3-10 µM, 26 days ) not affect on NSD2 knockout NPPO-1 and NPPO-2 organoids, has a slight effect on NSD2 knockout MSKPCa10[1].
NSD2-IN-6 (10 µM, 21 days) reduces H3K36me2 expression and modest upregulates H3K27me3 in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines, loss the lineage marker CD56 and upregulates AR in WCM1262 human CRPC organoid lines, results a reduction in organoid size and immunostaining for cleaved caspase 3 in MSKPCa2 organoids[1].
NSD2-IN-6 (0.3-10 µM, 21 days) lead a decreasing cell viability after enzalutamide treatment, a high Bliss synergy score and a concentration-dependent induction of apoptosis in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines when combinate with Enzalutamide [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NSD2-IN-6 Related Antibodies

Cell Viability Assay[1]

Cell Line: H3K27me3 in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 21 days
Result: Progressively decreased cell viability after enzalutamide treatment.

Apoptosis Analysis[1]

Cell Line: H3K27me3 in MSKPCa10, MSKPCa14, WCM154, WCM1262 and MSKPCa2 human CRPC organoid lines
Concentration: 0.3, 1, 3 and 10 μM
Incubation Time: 21 days
Result: Significantly increased caspase 3 and caspase 7 activity in a concentration-dependent manner.
In Vivo

NSD2-IN-6 (compound NSD2i) (75-300 mg/kg, p.o.,once daily for 5 days) reduces H3K36me2 levels in mice xenografts of human prostate organoids[1].
NSD2-IN-6 (150 mg/kg, p.o., daily for 42 days) exerts antitumor activity by by reversing plasticity, suppressing growth and promoting tumour cell apoptosis in mice xenografts of human prostate organoids[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Subcutaneous grafts of human CRPC organoids in NOD/SCID mice[1]
Dosage: 75, 150 and 300 mg/kg
Administration: p.o., daily for 5 days
Result: Reduced H3K36me2 levels at each con centration without any adverse effects on mouse body weights.
Animal Model: Subcutaneous grafts of human CRPC organoids in NOD/SCID mice[1]
Dosage: 150 mg/kg
Administration: p.o., daily for 42 days
Result: Had modest effects on tumour growth for MSKPCa10, MSKPCa14 and WCM1262 xenografts.
Resulted strong growth suppression when combined with Enzalutamide.
Displayed a strong responses when combined with or with not Enzalutamide.
Showed loss of neuroendocrine phenotypes accompanied by overt necrosis and fibrosis, and increased adenocarcinoma features in MSKPCa10, MSKPCa14 and WCM1262 xenografts when combine with Enzalutamide.
Showed Loss of H3K36me2 , neuroendocrine markers CHGA and SYP in MSKPCa10 and MSKPCa14, and loss of CD56 in WCM1262 when combined with Enzalutamide.
Displayed strong downregulation of Ki67 and upregulation of CC3 when combine with Enzalutamide.
Molecular Weight

546.52

Formula

C25H26F4N8O2
SMILES

NC1=NC=NC2=C1N=CN2CC3=CC(C4=C(F)C=C(OC)C(F)=C4)=NC=C3N5C[C@]([C@@H](O)C(F)F)(N)CCC5
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
References
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NSD2-IN-6 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NSD2-IN-6Histone Methyltransferaseorganoidsprostate cancerNSD2NSD1H3K36me2ARInhibitorinhibitorinhibit

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