anti-tumor

Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.

Niraparib (MK-4827) is a PARP inhibitor that selectively targets PARP1 and PARP2 (IC50=3.8 2.1 nM), exhibiting antitumor activity, inhibiting DNA damage repair, and inducing apoptosis.

Dipyrithione appears to have novel cytotoxicity and potent broad-spectrum antitumor activity

Niraparib, also know as MK-4827, is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. MK4827 inhibits PARP activity, enhancing the accumulation of DNA strand breaks and promoting genomic instability and apoptosis. The PARP family of proteins detect and repair single strand DNA breaks by the base-excision repair (BER) pathway.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

1. Ginkgetin has anti-influenza virus and anti-fungal activities. 2. Ginkgetin has anti-inflammatory activity, can down-regulates COX-2 induction in vivo against skin inflammatory responses. 3. Ginkgetin is a good STAT3 inhibitor and may be a useful lead

Naphthazarin (5,8-Dihydroxy-1,4-naphthoquinone) is effective by various cellular mechanisms including oxidative stress, activation of mitochondrial apoptosis-inducing factor (AIF), depolymerization of microtubules, interference with lysosomal function and p53-dependent p21 activation. It triggers apoptosis and has anti-tumor effects

AA-Z-YVAD-FMK is a Irreversible caspase-1 inhibitor,with anti-inflammatory and anti-tumor activities.

AES-135 is a potent HDAC inhibitor, inhibits HDAC3, HDAC6, HDAC11 (IC50s: 654, 190, and 636 nM) with anti-tumor activity.

Xanthone (Xanthenone) is currently used as ovicide for codling moth eggs and as a larvicide.

Niraparib hydrochloride (MK-4827 hydrochloride) is an inhibitor of poly (ADP-ribose) polymerase (PARP) with potential antineoplastic activity. By inhibiting PARP activity, niraparib hydrochloride increases DNA strand breaks, leading to genomic instability and apoptosis. The PARP family of proteins detects and repairs single-strand DNA breaks via the base-excision repair (BER) pathway.

(Rac)-Arnebin 1 (beta, beta-dimethylacrylshikonin) has anti-tumor, anti-inflammatory, anti-immune deficiency and protecting liver.

Niraparib tosylate (MK-4827 (tosylate))(with IC50 of 3.8 nM 2.1 nM) is a selective PARP1 PARP2 inhibitor.

Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR).

Isoscabertopin has anticancer activity.

Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).

MK-8033 is a new and selective dual ATP competitive c-Met Ron inhibitor (IC50: 1 nM Wt c-Met).

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

BMS-202 (PD1-PDL1 inhibitor 2) is an inhibitor of the PD-1 (Programmed death- 1) PD-Ll (Programmed death-ligand 1) protein protein interaction.

SR-717 is a cGAMP analog, a non-nucleoside STING agonist that induces a closed activation conformation of STING. SR-717 has antitumor activity and promotes activation of immune cells and cross-presentation of antigens.

Erythromycin (E-Mycin) is a Macrolide and Macrolide Antimicrobial. The physiologic effect of erythromycin is by means of Decreased Sebaceous Gland Activity.

Hesperidin (Cirantin) is a flavanone glycoside found in citrus fruits with antioxidant, anti-inflammatory, anti-carcinogenic, and antihypertensive and lipid-lowering activity.

Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.

Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.