基本信息

产品描述

Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation[1][2][3].

靶点（IC50 & Targe）

PKCδ3, μM (IC50, Porcine spleen)

PKCγ, 40 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCη, 82 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCε, 100 μM (IC50, baculovirus-infected Sf9 insect cells)

PKA, 78 μM (IC50, catalytic subunit from porcine heart)

PKCα, 30 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCβ, 42 μM (IC50, baculovirus-infected Sf9 insect cells)

PKCζ, 100 μM (IC50, baculovirus-infected Sf9 insect cells)

CKII, 30 μM (IC50, holoenzyme expressed in E.coli)

CaM kinase III, 5.3 μM (IC50, EF-2 kinase activity in cytosol of murine pancreas)

体外研究

Rottlerin (20 μM, 2/6/24 hours) dramatically decreases the cyclin D-1 mRNA levels in a time-dependent manner in primary HMVEC[2].

Rottlerin (20 μM) exhibits cell proliferation in HMVEC[2].

Western Blot Analysis[2]

体内研究

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[3].

Rottlerin inhibits tumor cell proliferation, and induces apoptosis through activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase (PARP)[3].

参考文献

[1]. Gschwendt M, et al. Rottlerin, a novel protein kinase inhibitor. Biochem Biophys Res Commun. 1994 Feb 28;199(1):93-8.

[2]. Valacchi G, et al. Rottlerin exhibits antiangiogenic effects in vitro. Chem Biol Drug Des. 2011 Jun;77(6):460-70.

[3]. Minzhao Huang, et al. Rottlerin suppresses growth of human pancreatic tumors in nude mice, and pancreatic cancer cells isolated from KrasG12D mice. Cancer Letters 353 (2014) 32-40.

安全信息

图形或危害标志
提示语	Warning
危险说明	H302
防范说明	P301+P312
WGK	3
RTECS	AM6913800

基本信息

Ref#
32849

MDL
17361

分子式
C30 H28 O8

分子量
516.6

产品说明

一般描述

A cell-permeable and reversible inhibitor of protein kinase C δ (PKCδ, IC₅₀ = 3-6 µM) and PKC_Θ isozymes. Also inhibits PKC_α, PKC_β, and PKC_γ isoforms, but with significantly reduced potency (IC₅₀ = 30-42 µM). Has reduced inhibitory activity on PKC_ε, PKC_η, and PKC_ξ (IC₅₀ = 80-100 µM). Also known to inhibit CaM kinase III (IC₅₀ = 5.3 µM).
A cell-permeable and reversible protein kinase C inhibitor that exhibits greater selectivity for PKC_δ (IC₅₀ = 3-6 µM) and PKC_θ. Inhibits the PKC_α, PKC_β, and PKC_γ isoforms, but with significantly reduced potency (IC₅₀ = 30-42 µM). Has reduced inhibitory activity on PKC_ε, PKC_η, and PKC_ζ (IC₅₀ = 80-100 µM). Also known to inhibit CaM kinase III (IC₅₀ = 5.3 µM).

包装

10 mg in Plastic ampoule

生化/生理作用

Cell permeable: yes
Product does not compete with ATP.
Primary Target
PKCδ
Reversible: yes
Target IC₅₀: 3-6 µM against PKCδ; 5.3 µM against CaM kinase III

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Villalba, M., et al. 1999. J. Immunol. 163, 5813.
Gschwendt, M., et al. 1994. Biochem. Biophys. Res. Commun. 199, 93.
Gschwendt, M., et al. 1994. FEBS Lett.338, 85.
Gschwendt, M., et al. 1984. Cancer Lett.25, 177.

法律信息

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

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation. H302 + H312 + H332: Harmful if swallowed, in contact with skin or if inhaled
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .