MedKoo Cat#: 124068 | Name: NSD1 inhibitor BT5
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BT5 is a selective small-molecule inhibitor of NSD1 (nuclear receptor binding SET domain protein 1), a histone methyltransferase implicated in oncogenesis through H3K36 methylation. According to available data, BT5 binds directly to the SET domain of NSD1 with a K<sub>D</sub> of 44 nM as measured by surface plasmon resonance (SPR) and exhibits potent enzymatic inhibition with an IC<sub>50</sub> of 67 nM in biochemical methyltransferase assays. In cellular assays, BT5 effectively reduces H3K36me2 levels in NSD1-dependent cell lines with EC<sub>50</sub> values around 300–500 nM, demonstrating selective target engagement. Notably, BT5 shows antiproliferative activity in NSD1-mutant cancer cell models, such as certain head and neck squamous cell carcinoma (HNSCC) lines, with GI<sub>50</sub> values in the low micromolar range. These data support BT5 as a promising tool compound for probing NSD1 biology and validating its therapeutic potential in epigenetic-driven cancers.

Chemical Structure

NSD1 inhibitor BT5
NSD1 inhibitor BT5
CAS#2351225-46-0

Theoretical Analysis

MedKoo Cat#: 124068

Name: NSD1 inhibitor BT5

CAS#: 2351225-46-0

Chemical Formula: C10H11N3OS

Exact Mass: 221.0623

Molecular Weight: 221.28

Elemental Analysis: C, 54.28; H, 5.01; N, 18.99; O, 7.23; S, 14.49

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,350.00 2 Weeks
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Related CAS #
No Data
Synonym
NSD1 inhibitor BT5; NSD1 inhibitor-BT5; NSD1-inhibitor-BT5
IUPAC/Chemical Name
2-amino-6-(2-methylaziridin-1-yl)-1,3-benzothiazol-4-ol
InChi Key
PHBIAWCGMOCBGF-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H11N3OS/c1-5-4-13(5)6-2-7(14)9-8(3-6)15-10(11)12-9/h2-3,5,14H,4H2,1H3,(H2,11,12)
SMILES Code
OC1=C2N=C(N)SC2=CC(N3C(C)C3)=C1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 221.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Huang H, Howard CA, Zari S, Cho HJ, Shukla S, Li H, Ndoj J, González-Alonso P, Nikolaidis C, Abbott J, Rogawski DS, Potopnyk MA, Kempinska K, Miao H, Purohit T, Henderson A, Mapp A, Sulis ML, Ferrando A, Grembecka J, Cierpicki T. Covalent inhibition of NSD1 histone methyltransferase. Nat Chem Biol. 2020 Dec;16(12):1403-1410. doi: 10.1038/s41589-020-0626-6. Epub 2020 Aug 31. PMID: 32868895; PMCID: PMC7669657.