Histone Methyltransferase Control

LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.

(S)-Bleximenib (oxalate) is a S-Enantiomer of Bleximenib oxalate (HY-148669A). Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC₅₀ values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia.

(2R)-Octyl-α-hydroxyglutarate (sodium) is the sodium salt form of (2R)-Octyl-α-hydroxyglutarate. (2R)-Octyl-α-hydroxyglutarate has anti-inflammatory effects.

(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.

UNC7145 is an inactive derivative of UNC6934 (HY-145103) that can be used as a negative control for the protein-protein inhibition activity of UNC6934.

MS8815N is a negative control of EZH2 PROTAC degrader MS8815 (HY-148334). MS8815N is incapable of recruiting the VHL E3 ligase but retains the same EZH2 binding moiety and linker. MS8815N can be used for triple-negative breast cancer (TNBC) research.

UNC-4219 TFA is a negative control for the CBX7-H3 antagonist UNC3866 (HY-100832) and does not interact with CBX7 at high concentrations.

LLY-284 (Standard) is the analytical standard of LLY-284 (HY-107777A). This product is intended for research and analytical applications. LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases.