| Cat. No. |
Product Name |
CAS No. |
Information |
| H9192 |
CRT0066854
|
1438881-19-6 |
CRT0066854 is a potent and selective atypical PKCs inhibitor. CRT0066854 is against full-length (FL) PKCι, PKCζ, and ROCK-II kinases with IC50 values of 132 nM, 639 nM, and 620 nM, respectively. |
| H8817 |
Darovasertib
|
1874276-76-2 |
Darovasertib is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research. |
| H7583 |
ζ-Stat
|
3316-02-7 |
ζ-Stat (1,3,6-Naphthalenetrisulfonic acid) is a novel PKC-zeta (PKC-ζ) specific inhibitor with IC50 of 5 uM, showed only 13%
inhibition on PKC-I at 20 uM; downregulates TNF-α induced NF-κB translocation to the nucleus there by inducing apoptosis, significantly decreases melanoma cell proliferation of SK-MEL-2 and MeWo. |
| H7582 |
UCN-01
|
112953-11-4 |
UCN-01 (7-Hydroxystaurosporine;NSC 638850) is a synthetic derivative of staurosporine that has antiproliferative activity against several in vitro and in vivo cancer models; inhibits a variety of kinases, including Akt, PKC (IC50=30 nM), PDK1 (IC50=6 nM), CDKs (IC50=300-600 nM for Cdk1 and Cdk2); arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by Chk1 (IC50=7 nM); induces apoptosis. |
| H7581 |
Sotrastaurin
|
425637-18-9 |
A potent, selective, orally available pan-PKC inhibitor with Ki of 0.22-3.2 nM for PKC isotypes; displays excellent selectivity against a broad panel of kinases (only GSK-3β IC50<1 uM); inhibits early T-cell activation with no general antiproliferative activity, also inhibits β2-integrin-mediated T-cell adhesiveness; prolongs rat heterotopic heart transplant survival in combination with adjunct immunosuppression agents. |
| H7580 |
Ruboxistaurin hydrochloride
|
169939-93-9 |
A potent, selective, ATP-competitive, orally available PKC beta (PKCβ) inhibitor with IC50 of 4.7 and 5.9 nM for PKCβ I and PKCβ II, respectively; displays >60-fold selectivity over PKCα, and other ATP dependent kinases (PKA, Calcium calmodulin, Caesin kinase and Src); ameliorates the glomerular filtration rate, albumin excretion rate, and retinal circulation in diabetic rats. |
| H7579 |
Roy-Bz
|
1246304-91-5 |
Roy-Bz is the first small-molecule PKCδ-selective activator with EC50 of 58.5 nM, binds to the PKCδ-C1-domain; displays no activity against human cPKCs (a mix of PKCα, β, and γ), nPKCδ, nPKCε and aPKCζ; potently inhibits the proliferation of colon cancer cells (HCT116 IC50=0.58 uM) by inducing a PKCδ-dependent mitochondrial apoptotic pathway involving caspase-3 activation; demonstrates PKCδ-dependent antitumor effect, through anti-proliferative, pro-apoptotic, and anti-angiogenic activities in xenograft mouse models with no apparent toxic side effects. |
| H7578 |
Rottlerin
|
82-08-6 |
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. |
| H7577 |
PZ09
|
1132609-87-0 |
PZ09 (PKC-zeta inhibitor 9, PKC-ζ inhibitor PZ9) is a potent, isoform selective PKC-zeta (PKC-ζ) inhibitor with IC50 of 5.18 nM, displays excellent selectivity (>200-fold) over other PKC isoforms with exception of PKC-i (10-fold); also shows high selectivity for CDK-2 (>200-fold), as well as a broader range of other kinases (
|
| H7576 |
PS-432
|
2083630-26-4 |
PS-432 is an allosteric inhibitor of PKCι and PKCζ with IC50 of 16.9 and 18.5 uM, respectively; has no inhibitory activity against PKCα, PKCβ, PKCδ and PKCθ nor the activity of related kinases such as PDK1, PKB/Akt, RSK1, MSK1 and Aurora A; inhibits the proliferation of the lung cancer cell lines A549 (IC50=14.8 ± 4.2 uM) and A427 (IC50=10.4± 0.3 uM) as well as androgen-independent prostate cancer cell line DU145 (IC50 = 20.8 ± 9.0 uM); well tolerated in vivo. |
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