99533-80-9
99533-80-9
Chemical Structure
K-252a
Synonym(s): SF2370; Antibiotic K 252a; Antibiotic SF 2370
- CAS No.: 99533-80-9
- Formula:C27H21N3O5
- Molecular Weight:467.47
IUPAC Name: methyl (5R,7R,8S)-7-hydroxy-8-methyl-15-oxo-5,6,7,8,14,15-hexahydro-13H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacene-7-carboxylate
InChIKey: KOZFSFOOLUUIGY-SOLYNIJKSA-N
SMILES: O=C(NC1)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5[C@](C[C@]7(O)C(OC)=O)([H])O[C@]7(C)N4C8=C3C=CC=C8
Biological Activity: K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively[1][2]. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene[3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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K-252a | 99.02% | K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene. | ||||||||||||||||||||
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CEP-1347 | 98.5% | CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53. | ||||||||||||||||||||
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TTT 3002 | TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research. | |||||||||||||||||||||
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NA0359 | NA0359 is a derivative of SF2370 (HY-N6732). NA0359 inhibits the actin-myosin-ATP interaction in native smooth muscle actomyosin and myosin light chain phosphorylation. | |||||||||||||||||||||
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NA 0345 | NA 0345 is a PKC inhibitor with IC50 values of 70 nM and 110 nM in the presence and absence of 12-O-tetradecanoyl-13-acetate, respectively. NA 0345 inhibits PKC and selectively suppresses the positive inotropic effect mediated by α1-adrenergic receptors. | |||||||||||||||||||||
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Lestaurtinib | 99.66% | Lestaurtinib (CEP-701) is an orally active and selective RPTKs (receptor protein tyrosine kinase) inhibitor, competitively inhibits ATP binding to the TrkA/B/C domain. Lestaurtinib inhibits RPTKs phosphorylation, with IC50s of 2, 25 and 0.9 nM for FLT3, TrkA and JAK2, respectively. Lestaurtinib induces apoptosis and cycle arrest, also can inhibit growth of tumor. | ||||||||||||||||||||
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Indocarbazostatin | Indocarbazostatin against Neurite outgrowth induced by NGF is 6 nM in rat pheochromocytoma PC12 cells. | |||||||||||||||||||||
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TAN-1030A | TAN-1030A is an indolocarbazole alkaloid with macrophage-activating properties. TAN-1030A induces spreading of a murine macrophage cell line, Mm 1, and augmentes the phagocytic activity, Fc gamma receptor expression and β-glucuronidase activity of murine macrophage cell lines, Mm 1 and J774A.1. TAN-1030A can activate macrophage functions in mice. | |||||||||||||||||||||
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K-252b | 99.66% | K-252b, an indolocarbazole isolated from the actinomycete Nocardiopsis, is a PKC inhibitor. K-252b can be used to inhibit extracellular kinases of cells in culture because it can’t pass through cell membrane freely . | ||||||||||||||||||||
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KT5720 | 98.53% | KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases. | ||||||||||||||||||||
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KT5823 | 99.9% | KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a Staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na+/I- symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation. | ||||||||||||||||||||
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References
- [1]. Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39(8), 1072-1078 (1986). [Content Brief]
- [2]. Davis, P.D., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides Journal of Medicinal Chemistry 35, 177-184 (1992). [Content Brief]
- [3]. Tapley P, et al. K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors. Oncogene. 1992 Feb;7(2):371-81. [Content Brief]
