Cancer Targeted Therapy

GNE-6893 is an orally active, selective HPK1 inhibitor with a K_i < 0.02 nM. GNE-6893 enhances T cell receptor signaling in primary human T cells. GNE-6893 increases IL2 production in stimulated primary human T cells. GNE-6893 can be used for the research of chronic refractory cancers.

KPZ560 is a potent inhibitor of HDAC1 and HDAC2, with IC₅₀s of 12 nM and 68 nM, respectively. KPZ560 can increase in the spine density of granule neuron dendrites of mice and inhibitor cell growth of breast cancer cell line MCF.

CCT 031374 hydrobromid is a potent inhibitor of β-catenin/transcription factor (TCF) complex signaling. CCT031374 inhibits TCF-dependent transcription of genes of Wnt signaling pathway. CCT 031374 has antitumor activity.

CZC-8004 (CZC-00008004) is a pan-kinase inhibitor. CZC-8004 has IC₅₀ values of 650 and 437 nM for EGFR WT and VEGFR2 V916M, respectively. CZC-8004 can be used in the study of cancer.

SENP2-IN-1 (compound 77) is a selective SENP2 inhibitor. SENP2-IN-1 shows inhibitory activities with IC₅₀s of 1.3, 0.69 and 22.7 μM for SENP1, SENP2 and SENP5, respectively. SENP2-IN-1 can be used for the research of cancer.

Necroptosis-IN-1, an analog of Necrostatin-1, is a potent necroptosis inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.

N-Demethyl Ivabradine (hydrochloride) is a metabolite of Ivabradine, which is a specific inhibitor of the funny channel.

4,4'-Dimethoxybenzil is a human intestinal carboxyl esterase (hiCE) inhibitor with K_i of 70 nM.

Methyltetrazine-PEG5-methyltetrazine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Methyltetrazine-PEG5-methyltetrazine is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.

(E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 (HY-12000) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

LIMK1 inhibitor BMS-4 is a LIM Kinase (LIMK) inhibitor targeting to LIMK1/2. LIMK1 inhibitor BMS-4 inhibits phosphorylation of cofilin, the LIMK substrate. However, LIMK1 inhibitor BMS-4 is noncytotoxic on A549 cells.

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC₅₀ of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC₅₀>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.

ERAP1 modulator-2 (compound 10) is a potent ERAP1 inhibitor with an IC₅₀ value of <100 nM.

Nodularin is a hepatotoxin, tumor promoter, and protein phosphatase inhibitor. Nodularin induces apoptosis (apoptosis) in normal cells (including caspase activation, upregulation of Bcl-XS, and upregulation of BAX/P53), triggers hyperphosphorylation of the MAPK/ERK, mTOR/S6K and p38 MAPK signaling pathways, and induces oxidative stress, endoplasmic reticulum membrane instability, peroxisome proliferation and increased lysosomal enzyme activity. Nodularin promotes DEN (HY-N7434)-initiated hepatocyte proliferation and adenoma formation, and inhibits proliferation, phagocytosis and chemotaxis of normal lymphocytes, oocyte maturation and vitellogenesis, as well as angiogenesis. Nodularin exhibits hepatotoxicity, reproductive and endocrine toxicity, and embryonic developmental toxicity in various animal models. Nodularin can be used in studies related to liver cancer, hepatotoxicity and reproductive endocrine toxicity.

Bcl-xL antagonist 2 is a potent, selective, and orally active antagonist of BCL-X_L with an IC₅₀ and K_i of 0.091 μM and 65 nM, respectively. Bcl-xL antagonist 2 promotes the apoptosis of cancer cells. Bcl-xL antagonist 2 has the potential for the research of the chronic lymphocytic leukemia (CLL) and non-Hodgkin’s lymphoma (NHL).

Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC₅₀s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo.

P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC₅₀ of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.

Mal-amido-PEG2-TFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Amino-PEG6-amido-bis-PEG5-N3 is a cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Amino-PEG6-amido-bis-PEG5-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

ALDOA-IN-1 is an aldolase A(ALDOA) inhibitor. ALDOA-IN-1 directly inhibits ALDOA enzymatic activity, thereby reducing lactate production, downregulating HIF-1α expression, and ultimately inducing cancer cell apoptosis. ALDOA-IN-1 can be used for research on colorectal cancer.