Src

A capsaicin analog with diverse biological activities

Phosphopeptide ligand for src SH2 domain

Syk inhibitor

UNC119 chaperone-cargo interaction inhibitor; disrupts Src activation

DGY-06-116 is an irreversible covalent, selective Src inhibitor with an IC50 of 3nM. DGY-06-116 inhibits FGFR1 with an IC50 of 8340 nM.

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

EPQpYEEIPIYL, a phosphopeptide, is a Src homology 2 (SH2) domain ligand. EPQpYEEIPIYL activates Src family members (e.g. Lck, Hck, Fyn) by binding to SH2 domains.

iHCK-37 (ASN05260065) is a potent and specific Hck inhibitor with a Ki value of 0.22 μM.

Caffeic acid-pYEEIE TFA, a non-phosphopeptide inhibitor, exhibits potent binding affinity for the GST-Lck-SH2 domain.

CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

YH-306 is an antitumor agent. YH-306 suppresses colorectal tumour growth and metastasis via FAK pathway. YH-306 significantly inhibits the migration and invasion of colorectal cancer cells. YH-306 potently suppresses uninhibited proliferation and induces cell apoptosis. YH-306 suppresses the activation of FAK, c-Src, paxillin, and PI3K, Rac1 and the expression of MMP2 and MMP9. YH-306 also inhibita actin-related protein (Arp2/3) complex-mediated actin polymerization.

HIV-IN-6 is a HIV-Ⅰ viral replication inhibitor by targeting Src family kinases (SFK) that interact with Nef protein of the virus, such as Hck.

Bosutinib (hydrate) is an orally available Src/Abl tyrosine kinase inhibitor with IC50 values of 1.2 nM and 1 nM, respectively.

LCB 03-0110, a thienopyridine derivative, is a potent pan-discoidin domain receptor/c-Src family tyrosine kinase inhibitor.

JNJ-49095397 (RV568) is an inhaled narrow-spectrum kinase inhibitor (NSKI) against both the α and γ isoforms of p38 MAPK.

Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor.

GW297361 is an oxindole CDK inhibitor that elicits a Pho85-selective response in cells.

BT424 is a specific HCK inhibitor.

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor.

PD173952 is a tyrosine kinases inhibitor with IC50s of 0.3, 1.7 and 6.6 nM against Lyn, Abl and Csk, respectively.

HPK1-IN-2 didrochloride is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity.

PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis.

KIN-8194 is an orally active dual inhibitor of HCK and BTK, with IC50 values of 0.915 and <0.495 nM, respectively.

DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase.