csr

CID-1067700 is one of the first identified competitive inhibitors of nucleotide binding by Ras-related GTPases(Rab7 with a Ki of 13 nM).

CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor), with a Kd of 7.43 µM in SPR assays, directly binding to the OC2-HOX domain. CSRM617 hydrochloride induces apoptosis through the appearance of cleaved Caspase-3 and PARP and is well tolerated in the mouse model of prostate cancer [1].

CSRM617 is a selective small molecule inhibitor of the transcription factor ONECUT2 (OC2, the main regulator of androgen receptor). The Kd in SPR analysis is 7.43 uM, which can directly bind to the OC2-HOX domain. CSRM617 induces apoptosis by cleaving the

cSRC/BCR-ABL1-IN-1 (compound 16a) is a dual-target inhibitor of the cSRC/BCR-ABL1 kinases.

cSRC/BCR-ABL-IN-1 (compound 21b) is a potent inhibitor of Bcr-Abl and C-Src, with IC50 values of 56.2 nM and 101 nM, respectively. It exhibits cytotoxicity.

Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.

Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.

LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.

Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.

Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).

Spermidine (N-(3-Aminopropyl)-1,4-diaminobutane) inhibits NOS1 (nNOS). Spermidine binds and precipitates DNA and may be used for purification of DNA binding proteins. Spermidine activates PNK (polynucleotide kinase T4). Spermidine binds to and activates NMDA and has been shown to potentiate NMDA-induced currents in a concentration-dependent manner.

Benidipine hydrochloride (Coniel) , a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.

AD57 is a potent inhibitor of both c-Src and Abl with IC50 of 0.025 μM and 0.041 μM, respectively.

YH-306 (TRV055 acetate ) is a modulator of the FAK signaling pathway that acts by suppressing colorectal tumor growth and metastasis.

NCGC00262650 is an inhibitor of AMA1-RON2 interaction and c-Src tyrosine kinase activity.

pp60 c-src (521-533) (phosphorylated) acetate is a regulator of focal adhesion formation and cell spreading. pp60 c-src (521-533) (phosphorylated) acetate also regulates cell motility and is a key component in the signaling pathway triggered by the motogenic hyaluronan receptor RHAMM.

KB SRC 4 is a selective and potent c-Src inhibitor with antitumour activity that inhibits the growth of cancer cells.

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC50 of 14.93 μM, effectively suppressing the proliferation of human gastric cancer cells by downregulating the PAK4/c-Src/EGFR/cyclin D1 pathway and inducing apoptosis.

Src Inhibitor 3 is an effective inhibitor of c-terminal Src kinase (IC50 <3 nM in CSK HTRF, <4 nM in Caliper assay). Src Inhibitor 3 increases T cell proliferation induced by T cell receptor signaling.

T338C Src-IN-1 is a potent inhibitor of the mutant Src T338C, exhibiting an IC50 of 111 nM relative to WT c-Src (showing a 10-fold increase).

T338C Src-IN-2 is a potent inhibitor of the mutant c-Src T338C kinase (IC50 of 317 nM), and it also inhibits T338C/V323A and T338C/V323S with IC50 values of 57 nM and 19 nM, respectively.

STAT-3/c-Src-IN-1 (Compound 12d) is a dual inhibitor of STAT-3 (IC50=0.844 μM) and c-Src (IC50=0.268 μM). It effectively disrupts tumor cell proliferation, migration, and angiogenesis pathways. This compound exhibits potent antiproliferative activity against melanoma (SK-MEL-2) and central nervous system cancer (SNB-75) cell lines, with GI50 values of -5.75 μM and -5.63 μM, respectively. It induces apoptosis through cell cycle arrest at the G0/G1 and G2/M phases. STAT-3/c-Src-IN-1 shows promise for research in melanoma and glioblastoma.

PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. It also inhibits the PDGFR, EGFR, and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.