Rottlerin

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Rottlerin (Mallotoxin;NSC 94525) 是一种多酚天然产物、细胞渗透性和可逆 PKC 抑制剂，对 PKCδ (IC50=3-6 uM) 和 PKCθ 表现出更高的选择性。

Rottlerin (Mallotoxin;NSC 94525) is a polyphenol natural product, cell-permeable and reversible PKC inhibitor that exhibits greater selectivity for PKCδ (IC50=3-6 uM) and PKCθ, with significantly reduced potency (IC50=30-42 uM) for PKCα, PKCβ, and PKCγ; also inhibits CaMK III, suppresses eEF-2 phosphorylation with IC50 of 5.3 uM; also remarkably inhibits MACC1 promoter activity and expression, reduces cell motility in CRC cells.

Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC.Rottlerin (20 μM) exhibits cell proliferation in HMVEC. Western Blot Analysis Cell Line:Primary HMVEC (Human Microvascular Endothelial Cell).Concentration:20 μM.Incubation Time:2, 6, 24 hours.Result:Dramatically decreased the cyclin D-1 mRNA levels in a time-dependent manner. After 2 h of treatment, the mRNA level was reduced to 50% of the control, to circa 40% after 6 h, and to 20% after 24 h. Consistently, a similar trend was observed in the protein levels, where the decrease was circa 50% after 2 h, 80% after 6 h, and to almost undetectable levels after 24 h.Cell Proliferation Assay Cell Line:Primary HMVEC (Human Microvascular Endothelial Cell).Concentration:20 μM.Incubation Time:24/48 hours.Result:Exhibited a strong growth inhibition, with a reduction in thymidine incorporation respect to the control cells (DMSO 0.1%) of circa 75% and 80%, respectively.

Rottlerin (20 mg/kg, gavage 5 days per week, once daily, for 6 weeks) inhibits AsPC-1 pancreatic tumor growth in Balb C nude mice with no toxicity.Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP). Animal Model:Balb C nude mice (4-6 weeks old) with AsPC-1 cells (2×106 cells mixed with Matrigel, 50:50 ratio) injection.Dosage:0 or 20 mg/kg.Administration:Gavage 5 days per week, once daily, for 6 weeks.Result:Inhibited AsPC-1 pancreatic tumor growth in Balb C nude mice and had no effect

Mallotoxin | NSC 94525

Angiogenesis

PKC

PKC

Other Indications

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82-08-6

516.54

C30H28O8

>98% (HPLC)

DMSO : 2 mg/mL 3.87 mM;H2O : < 0.1 mg/mL

CC1(C)C=CC2=C(O)C(CC3=C(C(C)=C(C(C(C)=O)=C3O)O)O)=C(O)C(C(/C=C/C4=CC=CC=C4)=O)=C2O1

(2E)-1-[6-[(3-acetyl-2,4,6-trihydroxy-5-methylphenyl)methyl]-5,7-dihydroxy-2,2-dimethyl-2H-1-benzopyran-8-yl]-3-phenyl-2-propen-1-one

(-20℃)

With Ice Pack

≥ 2 years