5.31996

KDM4A/KDM4B Inhibitor, NSC636819

• 동의어(들): KDM4A/KDM4B Inhibitor, NSC636819, JMJD2 Inhibitor, Jumonji C-containing Histone Lysine Demethylase Inhibitor
• 실험식(Hill 표기법): C₂₂H₁₂Cl₄N₂O₄
• CAS Number: 1618672-71-1
• Molecular Weight: 510.15
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: solid
• 효능: 3.0 μM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: brown
• solubility: DMSO: 10 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC₅₀ = 6.4 µM; K_i = 5.5 µM) and KDM4B (IC₅₀ = 9.3 µM; K_i = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC₅₀ = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.

A cell permeable dinitrobenzene derivative that acts as a competitive inhibitor of KDM4A (IC₅₀ = 6.4 µM; K_i = 5.5 µM) and KDM4B (IC₅₀ = 9.3 µM; K_i = 3.0 µM) and completely blocks their demethylating activity toward H3K9me3 (~ 5 µM). Exhibits much reduced activities against KDM4D and KDM4E. Effectively induces apoptosis in LNCaP cells (IC₅₀ = 16.5 µM after 3-day culture), but does not affect normal PNT2 cells (~ 5 to 20 µM over 6 days). Shown to up-regulate RB1 and CDH1 tumor suppressor genes and down-regulates IGF1R, FGFR3, CCNE2, AURKA, and AURKB oncogenes.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
KDM4A/B

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 3 months at -20°C.

기타 정보

Chu, C.H., et al. 2014. Journ. Med. Chem.57, 5975.

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