WM-3835
WM-3835 Basic information
- Product Name:
- WM-3835
- Synonyms:
-
- WM-3835
- invasion,MYST2,HBO1,WM3835,MYLK-HOXA9,Histone Acetyltransferase,Apoptosis,inhibit,H4K12ac,HATs,KAT7,WM-3835,migration,WM 3835,acetyl-CoA,HAT,OS) cell proliferation,osteosarcoma,H3K14ac,Inhibitor,pOS-1
- N'-(4-Fluoro-5-methyl-[1,1'-biphenyl]-3-carbonyl)-3-hydroxybenzenesulfonohydrazide
- [1,1'-Biphenyl]-3-carboxylic acid, 4-fluoro-5-methyl-, 2-[(3-hydroxyphenyl)sulfonyl]hydrazide
- WM-3835, 10 mM in DMSO
- CAS:
- 2229025-70-9
- MF:
- C20H17FN2O4S
- MW:
- 400.42
- Mol File:
- 2229025-70-9.mol
WM-3835 Chemical Properties
- Density
- 1.369±0.06 g/cm3(Predicted)
- storage temp.
- 4°C, protect from light
- solubility
- DMSO : 250 mg/mL (624.34 mM; Need ultrasonic)
- pka
- 7.26±0.25(Predicted)
- form
- Solid
- color
- White to off-white
WM-3835 Usage And Synthesis
Uses
WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice[1].
Biological Activity
WM-3835is a cell-permeable hydroxybenzenesulfonohydrazide compound th at acts as a potent, selective, Ac-CoA competitive and reversible inhibitor of HBO1, KAT6A, and TIP60 acetyltransferases (IC50 = 0.030, 0.017 and 0.312 μM, respectively). WM-3835 is non-cytotoxic, dose-dependently, and rapidly decreases H3K14Ac levels (IC50 = 0.341 μM) and inhibits AML cells growth (IC50 = 0.297 μM in Molm13). Induces apoptosis, downregulates HOXA and IL-6 expression and up-regulates ALB secretion and delays hepatocyte and hMPC senescence. WM-1385 potently inhibits POS-1 xenograft growth in SCID mice (10 mg/kg, i.p.).
in vivo
WM-3835 (10 mg/kg/day; ip; for21 days) potently inhibits pOS-1 xenograft growth in SCID mice[1].
| Animal Model: | SCID mice (18-19 g, female) with pOS1 cells[1] |
| Dosage: | 10 mg/kg |
| Administration: | IP; daily; for 21 days |
| Result: | Potently inhibited pOS-1 xenograft growth. |
IC 50
HBO1
storage
Store at -20°C
References
[1] Yan-Yang Gao, et al. The histone acetyltransferase HBO1 functions as a novel oncogenic gene in osteosarcoma. Theranostics. 2021 Mar 4;11(10):4599-4615. DOI:10.7150/thno.55655
WM-3835Supplier
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