2561494-77-5
Chemical Structure
UNC6934
- No. CAS: 2561494-77-5
- Formula:C24H21N5O4
- Molecular Weight:443.45
IUPAC Name: N-cyclopropyl-3-oxo-N-(4-(pyrimidin-4-ylcarbamoyl)benzyl)-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide
InChIKey: KOZGEDUWAQFVAV-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C(CN(C2CC2)C(C3=CC=C4NC(COC4=C3)=O)=O)C=C1)NC5=CC=NC=N5
Biological Activity: 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[1][2].
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UNC6934 | 98.24% | 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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References
- [1]. Dilworth D, et al. A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. Nat Chem Biol. 2022;18(1):56-63. [Content Brief]
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[2]. James Stafford, et al. Examining the in-vitro effect of UNC6934 & BI-9321 alone and in combination with ONC201 on Diffuse Intrinsic Pontine Glioma (DIPG) cells. May 2nd, 2022.
