hck

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).

Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.

TL02-59 dihydrochloride is an orally active inhibitor of the Src-family kinase Fgr, with an IC50 of 0.03 nM.

iHCK-37 (ASN05260065) is a selective Hck inhibitor with antitumor activity, blocking HIV-1 viral replication. iHCK-37 reduces PI3K/AKT and MAPK/ERK pathway activation after erythropoietin induction in high Hck-expressing cells, useful in chronic myelogenous leukemia (CML) research.

Hck-IN-2 (Compound 8e) acts as an HCK inhibitor with demonstrated cytotoxic effects on tumor cells. It exhibits an IC50 of 19.58 μM for MDA-MB231 cells and 1.42 μM for MCF-7 cells. Additionally, Hck-IN-2 possesses antitumor activity.

Hck-IN-3 is an orally effective inhibitor targeting HCK with a KD of 3.92 μM. It suppresses the release of NO and exhibits an IC50 of 6.52 μM in RAW264.7 cells. Hck-IN-3 inhibits the release of TNF-α, IL-6, and IL-1β in a concentration-dependent manner. Additionally, it downregulates the protein expression of NLRP3, ASC, pro-caspase-1, and pro-IL-1β, also dependent on concentration. Hck-IN-3 is applicable for research into acute and non-injury related inflammatory diseases.

DFCI-002-06 is an orally active dual-targeted HCK/BTK PROTAC degrader, demonstrating DC₅₀ values of 1.3 nM for HCK and 4.5 nM for BTK. It retains superior antitumor activity compared to dual-targeted HCK/BTK inhibitors and induces apoptosis in cancer cells. DFCI-002-06 is applicable in studies of MYD88-mutant B-cell malignancies.

Torkinib (PP 242) (PP 242) is a selective and ATP-competitive mTOR inhibitor (IC50: 8 nM). It also inhibits mTORC1/2 (IC50s: 30/58 nM).

BMS-243117 is an effective selective LCK inhibitor with good cell activity (IC(50)=1.1 microM) and inhibition of T cell proliferation, which has great potential for therapeutic immunosuppression and the treatment of diseases such as rheumatoid arthritis a

Pyridone 6 (JAK Inhibitor)(CMP 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.

TG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

HIV-IN-6 is an HIV viral inhibitor that inhibits the replication of the HIV virus.HIV-IN-6 has anti-HIV viral activity and works by targeting Src family kinases (SFK) (e.g., Hck) that interact with the viral Nef protein.

TG 100572 is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).

TG 100801 Hydrochloride is a prodrug to treat age-related macular degeneration. TG 100572 is a inhibitor of multi-targeted kinase(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src,

MRT-10350 (Compound 2) is a cereblon-based molecular glue degrader targeting HCK. This compound is applicable for research in diseases such as chronic myelogenous leukemia and HIV-1 infection.

MRT-7612 (Compound 4) is a cereblon-based molecular glue degrader targeting tyrosine kinases. It significantly induces the degradation of HCK and LYN, with a comparatively weaker effect on LCK. MRT-7612 is applicable in research related to cancers such as chronic myeloid leukemia, autoimmune disorders, and chronic inflammatory diseases.

SIK1-IN-1 (Compound 27) is a selective inhibitor of salt-inducible kinase 1 (SIK1) with an IC50 of 0.7 nM, demonstrating greater potency for SIK1 compared to SIK2 and SIK3. It shows no cytotoxicity in HEK293 cells and PBMC at concentrations up to 30 μM. Additionally, SIK1-IN-1 effectively inhibits 392 kinases, particularly tyrosine kinases such as FGR, HCK, and LYN.

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

EPQpYEEIPIYL, a phosphopeptide, is a ligand for the Src homology 2 (SH2) domain, activating Src family members such as Lck, Hck, and Fyn through binding interactions with SH2 domains.

AZD-7762, an effective and specific inhibitor of Chk1(IC50=5 nM), is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.

(Z)-LFM-A13(IC50=2.5 μM), a specific Bruton's tyrosine kinase (BTK), is more than 100-fold specificity than other protein kinases, such as JAK1, JAK2, HCK, EGFR, and IRK.

BT424, a specific HCK inhibitor, modulates macrophage activation and autophagy in vitro, and mitigates inflammation and renal fibrosis in the UUO model [1].