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ZINC69391

  Cat. No.:  DC43389   Featured
Chemical Structure
303094-67-9
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More than 5000 active chemicals with high quality for research!
Field of application
Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 303094-67-9
Chemical Name: 2-(4,6-Dimethylpyrimidin-2-yl)-1-[2-(trifluoromethyl)phenyl]guanidine
Synonyms: 2-(4,6-dimethylpyrimidin-2-yl)-1-[2-(trifluoromethyl)phenyl]guanidine;N'-(4,6-dimethylpyrimidin-2-yl)-N-[2-(trifluoromethyl)phenyl]guanidine;N-(4,6-Dimethyl-2-pyrimidinyl)-N'-[2-(trifluoromethyl)phenyl]-guanidine;SMSF0013930;CB12619;Z56785930
SMILES: FC(C1=C([H])C([H])=C([H])C([H])=C1N([H])C(N([H])[H])=NC1=NC(C([H])([H])[H])=C([H])C(C([H])([H])[H])=N1)(F)F
Formula: C14H14F3N5
M.Wt: 309.2897
Purity: >98%
Sotrage: 0°C (short term), -20°C (long term), desiccated
Description: Novel specific Rac1 inhibitor, interferring with the interaction of Rac1 with Dock180, a relevant Rac1 activator in glioma invasion, and to reduce Rac1-GTP levels
In Vivo: ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model[3]. Animal Model: Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)[3] Dosage: 25 mg/kg body weight Administration: I.p; daily for 21 days Result: Significantly reduced by about 60% the formation of total metastatic lung colonies.
In Vitro: ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM[1]. ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner[1]. ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells[2]. ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest[2]. ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells[1]. Cell Proliferation Assay[2] Cell Line: U-87 MG, LN229 cells Concentration: 0-125μM Incubation Time: 72 hours Result: Reduced cell proliferation in a concentration-dependent manner. Cell Cycle Analysis[2] Cell Line: LN229 cells Concentration: 50, 100 μM Incubation Time: 48 hours Result: Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner. Apoptosis Analysis[1] Cell Line: HL-60, U937 and KG1A cell lines Concentration: 50 μM Incubation Time: 24 hours Result: Led to a significant increase in apoptotic cells.
References: [1]. Cabrera M, et al. Pharmacological Rac1 inhibitors with selective apoptotic activity in human acute leukemic cell lines. Oncotarget. 2017;8(58):98509‐98523. Published 2017 Oct 4. [2]. Cardama GA, et al. Proapoptotic and antiinvasive activity of Rac1 small molecule inhibitors on malignant glioma cells. Onco Targets Ther. 2014;7:2021‐2033. Published 2014 Oct 30. [3]. Cardama GA, et al. Preclinical development of novel Rac1-GEF signaling inhibitors using a rational design approach in highly aggressive breast cancer cell lines. Anticancer Agents Med Chem. 2014;14(6):840‐851.
MSDS
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COA
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Cat. No. Product name Field of application
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC74583 ZK53 ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins.
DC74576 Fluorofurimazine Fluorofurimazine is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine enables higher substrate loading and improved optical imaging sensitivity in in-vivo.
DC74557 PREX-in1 PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
DC74555 GYS32661 GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
DC74539 L557-0155 L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.
DC74528 K284 K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.
DC74247 AG-946 AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
DC74225 YB-537 YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).
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