wt-1

WT-1 A1 is an attractive target for immunotherapy in patients with pancreatic adenocarcinoma.

Grisnilimab (WT1) is a monoclonal antibody targeting CD7. CD7 plays a crucial role in T cell and T cell/B cell interactions, and the Wilms' tumour 1 (WT1) gene is overexpressed in leukaemia and various types of solid tumours (such as lung cancer and colorectal cancer).

Grisnilimab setaritox (WT1-RTA), an anti-CD7 antihuman T cell antibody linked to ricin A chain (RTA), exhibits in vitro cytotoxicity against CEM (T-lymphoblastic leukemia) cells with an ID 50 of 53 pM. The 30-kDa RTA component disrupts the function of 60S ribosomal subunits. Additionally, Grisnilimab setaritox has demonstrated efficacy in ameliorating leukemic meningitis in a rhesus monkey model [1].

WT1 126-134 peptide is a WT1 polypeptide (Wilms' tumor 1 peptide) (RMFPNAPYL) that activates cytotoxic CD8 T cells to target and destroy WT1+ tumor cells. It can form stable complexes with either H-2Db (murine) or HLA-A0201 (human) molecules. The WT1 126-134 peptide/HLA-A0201 complex exhibits high affinity for humanized monoclonal antibodies (IgG1), with a dissociation constant (Kd) of 0.2 nM. This peptide can be utilized as a T cell vaccine or an antibody target.

WT161 is a potent and selective inhibitor of HDAC6 (IC50:0.40 nM).

Zandelisib is an inhibitor of phosphatidylinositol 3-kinase (PI3K)(p110δ, IC50 of 3.5 nM), and with antineoplastic activity.

P110δ-IN-1 (PWT-143) is an effective and selective inhibitor of P110δ (IC50: 8.4 nM).

Zandelisib (ME-401) hydrochloride is a selective, orally active, non-covalent PI3Kδ inhibitor. It effectively and persistently inhibits AKT phosphorylation and downstream signaling pathways. Zandelisib hydrochloride is utilized in research on malignant tumors such as relapsed/refractory B-cell lymphoma.

E1210 (APX001A) is broad-spectrum and orally active antifungal

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. It exhibits activity against the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM), and EGFR wt (IC50=190 nM). BI-4020 also shows high kinome selectivity and good DMPK properties.

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

Zongertinib is a human HER2-selective tyrosine kinase inhibitor, a novel TK that is highly selective for covalent binding to the HER2 tyrosine kinase domain (TKD).Zongertinib exhibits antitumor activity with inhibitory effects on pHER2 and EGF.

Sonrotoclax is a potent, orally active inhibitor of Bcl2, demonstrating effective cell-killing activity against a range of lymphoma and leukemia cell lines [1].

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.

Darunavir Ethanolate (UIC 94017) is an HIV PROTEASE INHIBITOR that is used in the treatment of AIDS and HIV INFECTIONS. Due to the emergence of ANTIVIRAL DRUG RESISTANCE when used alone, it is administered in combination with other ANTI-HIV AGENTS.

Mutant IDH1-IN-1 is a potent inhibitor of the mutant IDH1 R132 h, exhibiting an IC50 of less than 0.1 μM.

K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).

EGFR-IN-7 (TQB3804) is a selective and potent EGFR kinase inhibitor.

GSK3532795 is a potent, orally active, second-generation HIV-1 maturation inhibitor (EC50s: 10.2, 1.9, 2.7, and 13 nM for HIV-1 WT(human serum), HIV-1 WT, HIV-1 V370A, and HIV-1 ΔV370).

MtbHU-IN-1 is a Mycobacterium tuberculosis nucleoid-associated protein HU (MtbHU)inhibitor(binding to WT MtbHU with a Kd of 98 nM).

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).

CD38 inhibitor 1 is a potent CD38 inhibitor that is effective against human CD38 (IC50 value is 7.3 nM) and mouse CD38 (IC50 value is 1.9 nM).