Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. Tubastatin A is a very selective HDAC6 inhibitor with 100 to over 1000-fold selectivity for HDAC6 over other HDAC classes. Tubastatin A increases the total numbers of mitochondria and restores the number of moving mitochondria in DRG neurons. It reverses the axonal loss in peripheral neurons in the mouse model of Charcot-Marie-Tooth disease. Tubastatin A inhibits the deacetylation of α-tubulin in murine myoblasts.

Chelerythrine is a kind of benzo[c] phenanthridine alkaloids, which is widely found in plant of Fumariaceae, Papaveraceae, Ranunculaceae and Rutaceae families. Chelerythrine is a potent and specific inhibitor of protein kinase C. In addition chelerythrine inhibits pro-survival protein Bcl(XL) thereby inducing apoptosis. It exerts antitumor properties.

SB-202190 is a potent inhibitor of MAPK14 and MAPK11. It has been investigated in a number of preliminary cell-based studies including several cancer models. SB-202190 has been shown to be a UVB protectant; SB-202190 strongly inhibits UVB induced COX-2 protein expression in HaCaT cells and markedly inhibits UVB induced cox-2 mRNA. SB-202190 induces apoptosis through activation of CPP32-like caspases. SB-202190 has been studied in animal models of the Renal Fibrosis and Pemphigus Vulgaris. It should be noted that in vivo use is most effective (at least for renal fibrosis) when SB-202190 is conjugated to lysozyme using a universal linkage system.

MRT 67307 dihydrochloride is a novel inhibitor of IKK-epsilon/TBK1. Negative regulation on the canonical IKKs may be critical in preventing the overproduction of the inflammatory mediators that lead to inflammatory and autoimmune diseases. In addition, it was demonstrated that MRT 67307 inhibits series of MARKs and salt inducible kinases (SIKs). SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and other anti-inflammatory molecules. It is an inhibitor for ULK1and ULK2. ULK1, a serine/threonine protein kinase, is essential for the initial stages of autophagy. Cancer cells are thought to take advantage of autophagy to help them to cope with the stress of tumorigenesis; thus targeting autophagy is an attractive therapeutic approach.

Diphenyl acetamidotrichloroethyl fluoronitrophenyl thiourea, CGK733, was claimed to be selective inhibitor of the ataxia telangiectasia-mutated (ATM) protein and ATM- and Rad3-related (ATR) protein, however after investigation of the contents of the original paper by Korean Advanced Institute of Science and Technology (KAIST) several irregularities has been revealed and the paper was retracted in full. Further studies were completed showing that CGK-733 has no specific inhibitory effect on ATM or ATR. Unfortunately, the compound is still being marketed as an ATM/ATR inhibitor. CGK733 inhibits the proliferation of human cancer and non-transformed mouse fibroblast cell lines and induced senescent breast, lung, and colon carcinoma cells to undergo cell death.

KU-55933 (2-morpholin-4-yl-6-thianthren-1-yl-pyran-4-one) is an ATP-competitive inhibitor of Ataxia telangiectasia mutated (ATM) kinase. Exposure of cells to KU-55933 resulted in a significant sensitization to the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents, etoposide, doxorubicin, and camptothecin. Inhibition of ATM by KU-55933 also caused a loss of ionizing radiation-induced cell cycle arrest. By contrast, KU-55933 did not potentiate the cytotoxic effects of ionizing radiation on ataxia-telangiectasia cells, nor did it affect their cell cycle profile after DNA damage. KU55933 is a hydrophobic molecule and is insoluble in water. Nanoparticle KU55933 is a potent radiosensitizer in vitro using clonogenic assay and is more effective as a radiosensitizer than free KU55933 in vivo using mouse xenograft models of non-small cell lung cancer (NSCLC).

PP121 is a multitargeted dual receptor tyrosine kinases inhibitor. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases. PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases.

KRN633 is a selective inhibitor of Vascular endothelial growth factor receptors VEGFR-1, -2, and -3. KRN633 also blocked the activation of mitogen-activated protein kinases by VEGF, along with human umbilical vein endothelial cell proliferation and tube formation. KRN633 inhibited tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. Kirin Brewery developed angiogenesis inhibitor KRN 633 as a treatment for solid tumours. It is in phase I clinical trials.

AZD2932 is an oral inhibitor of VEGFR-2 and PDGFR tyrosine kinases, which was developed by AstraZeneca as a potential anti-cancer medicine. The drug was tested in vivo in preclinical model of mice bearing C6 rat glial tumors and AZD2932 demonstrated good potency: growth of Calu-6 tumor was inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and LoVo tumors by 67% at 50 mg/kg b.i.d.

Cinnamtannin B-1 is a naturally occurring A-type proanthocyanidins, available in a limited number of plants, including C. zeylanicum and L. nobilis, that exhibit a large number of cellular actions mostly derived from its antioxidant activity, including antitumoral activity mediated by a selective pro-apoptotic action in a number of tumoral cell lines associated with a remarkable antiapoptotic activity in normal cells. In addition, cinnamtannin B-1 shows antithrombotic actions through inhibition of platelets' endogenous ROS generation, Ca2 mobilization and subsequently aggregation. This has been reported to be especially relevant in platelets from diabetic patients where cinnamtannin B-1 reverses both platelet hypersensitivity and hyperactivity. Considering the large number of cellular effects of cinnamtannin B-1, this compound might be further investigated for the development of therapeutic strategies based on its use for thrombotic disorders or certain types of cancer. Cinnamtannin B-1 is a potent antioxidant and protective agent against oxidative stress and apoptosis in human platelets. Cinnamtannin B-1 is a Cox-2 (cyclooxygenase-2) inhibitor. Cinnamtannin B1 was a potent cancer cell proliferation inhibitor and a good intracellular antioxidant.