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FN-1501 is a potent FLT3 and CDK inhibitor (IC50s: 2.47, 0.85, 1.96, and 0.28 nM for CDK2/cyclin A, CDK4/cyclin D1, CDK6/cyclin D1 and FLT3, respectively). FN-1501 also has anticancer activity.
SP-8356 is a potent, orally active inhibitor of cluster of differentiation 147 (CD147) with anti-atherosclerotic effects.
CP 31398 dihydrochloride is a p53 stabilizer which stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53.
RIPK1-IN-7 is a potent and selective inhibitor of RIPK1(Kd of 4 nM and an enzymatic IC50 of 11 nM), andexhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model.
Pyridone 6 is a potent and selective inhibitor of JAK1 (IC50=15 nM, murine JAK1), JAK2 (IC50=1 nM), JAK3 (Ki=5 nM), and Tyk2 (IC50=1 nM); displaying significantly weaker affinities (130 nM to 10 mM) for other protein tyrosine kinases.
Thapsigargin is a microsomal Ca2+-ATPase inhibitor and Endoplasmic Reticulum stress-inducing agent.
Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.
Indisulam is a carbonic anhydrase inibitor and Antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition.
Bisindolylmaleimide VIII acetate is a potent and selective PKC inhibitor (IC50: 158 nM for rat brain PKC). It has IC50s of 53, 195, 163, 213, and 175 nM for PKC-, PKC-I, PKC-II, PKC-, PKC-, respectively.
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol is 1000 times more selective for ErbB2 (IC50=3.4 M) and a range of other related tyrosine kinases (IC50 >>10 M). Falnidamol is a pyrimidine-pyrimidine compound with anti-cancer activity.
Cerdulatinib is an novel oral dual Syk/JAK inhibitor.
JAK2 inhibitor G5-7 is an orally active JAK2 inhibitor, selectively inhibits JAK2mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 has the potential for glioma study.
Concanavalin A is a plant lectin that is a T cell mitogen. It induces apoptosis in human fibroblasts.
Gossypol-acetic acid, a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.
1-Naphthyl PP1 hydrochloride is a selective inhibitor of src family kinases v-Src.
Oglufanide is a naturally occurring thymic immunomodulator, and inhibits vascular endothelial growth factor (VEGF).
Verteporfin, a benzoporphyrin derivative monoacid ring A, can inhibit the activity of YAP.
Pomalidomide inhibits TNF- release in LPS stimulated human PBMCs (IC50: 13 nM). It is an anti-angiogenic agent and an immunomodulator.
