420205

Histone Lysine Demethylase Inhibitor VIII, GSK-J4

Histone Lysine Demethylase Inhibitor VIII, GSK-J4, CAS 1373423-53-0, is converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (~ 25 to 50 µM in HeLa cultures).

• 동의어(들): Histone Lysine Demethylase Inhibitor VIII, GSK-J4, GSK-J1 Pro-Drug, JHDM Inhibitor II Pro-Drug, Ethyl-3-(6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-2-yl)pyrimidin-4-ylamino)propanoate
• 실험식(Hill 표기법): C₂₄H₂₇N₅O₂
• CAS Number: 1373423-53-0
• Molecular Weight: 417.50
• MDL number: MFCD22683852
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥98% (HPLC)
• 형태: semisolid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: tan
• solubility: DMSO: 100 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C
• InChI: 1S/C24H27N5O2/c1-2-31-23(30)10-14-26-21-17-22(28-24(27-21)20-9-5-6-13-25-20)29-15-11-18-7-3-4-8-19(18)12-16-29/h3-9,13,17H,2,10-12,14-16H2,1H3,(H,26,27,28)
• InChI key: WBKCKEHGXNWYMO-UHFFFAOYSA-N

설명

일반 설명

A cell-permeable GSK-J1 (Cat. No. 420204) prodrug that is ineffective in cell-free assays, but is effectively converted to GSK-J1 intracellularly for effective JMJD3 and UTX inhibition (effective conc. 25 to 50 µM in HeLa cultures). GSK-J4 treatment is shown to block LPS-induced TNF-α production in primary human macrophage cultures (IC₅₀ = 9 µM by ELISA).


This probe is supplied in conjunction with the Structural Genomics Consortium (SGC). For further characterization details, please visit the SGC website (http://www.thesgc.org/scientists/chemical_probes/GSKJ1).

The H3K27me3 demethylase inhibitor GSK-J1 (Cat. No. 420204) against JMJD3 and UTX is made cell-permeable by ethyl ester derivatization to facilitate cellular delivery ([medium GSK-J4]_t=0 = 30 µM; [cellular GSK-J1]_t=1h = 1.6 µM). The pro-drug GSK-J4, being ineffective in cell-free assays, is effectively converted to GSK-J1 intracellularly and inhibits nuclear H3K27me3 levels in both untransfected and JMJD3-transfected HeLa cells (25 to 50 µM). Simultaneous inhibition of cellular JMJD3 and UTX by GSK-J4 treatment is shown to block LPS-induced production of several proinflammatory cytokines, including TNF-α (IC₅₀ = 9 µM by ELISA), in primary human macrophage cultures.

생화학적/생리학적 작용

Cell permeable: yes

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months for -20°C.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable