RLY01 | REGγ-20S proteasome inhibitor | Probechem Biochemicals

Chemical Structure : RLY01

加入收藏

RLY01 (RLY-01)

货号: PC-24244Not For Human Use, Lab Use Only.

RLY01 is a potent small-molecule REGγ-20S proteasome inhibitor, has affinity (KD) of 11.6 uM for 20S proteasome, blocks its degradation function, ultimately leading to cancer cell death.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

RLY01 is a potent small-molecule REGγ-20S proteasome inhibitor, has affinity (KD) of 11.6 uM for 20S proteasome, blocks its degradation function, ultimately leading to cancer cell death.
RLY01 binds to and occupies the REGγ-bound pocket, suppressing REGγ-dependent 20S proteasome activity.
RLY01 blocks the degradation function of the REGγ-20S proteasome in a REGγ-dependent manner.
RLY01 blocks the growth of pan-KRAS–mutant tumors in vitro.
RLY01 increases the levels of the apoptosis-related proteins cleaved PARP (Cl-PARP) and cleaved caspase-3 (Cl-caspase-3) in KRAS-mutant cells in a concentration-dependent and REGγ-dependent manner, with no substantial effect on apoptosis in HCT116-REGγ-KO cells.
RLY01 treatment (25-50 mg/kg) effectively suppressed tumor growth in KRAS-mutant cancer models and lung cancer organoids.
The combination of RLY01 and the KRASG12C inhibitor AMG510 exhibited enhanced antitumor efficacy in KRASG12C cancer cells.

物理化学性质&存储条件

分子量	408.84
分子式	C21H17ClN4O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-amino-4-(3-((4-chlorophenoxy)methyl)-4-methoxyphenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

参考文献

1. Shen S, et al. J Clin Invest. 2025 Mar 17;135(6):e185278.

RLY01 (RLY-01)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

RLY01 (RLY-01)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.