4-4 cell

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Oxaliplatin (L-OHP) is a DNA alkylating agent and DNA synthesis inhibitor. Oxaliplatin induces cellular autophagy and DNA cross-linking damage, thereby inhibiting DNA replication and transcription and leading to cell death. Oxaliplatin is unstable in chlorine-containing systems; dissolution in saline or PBS is not recommended. A 5% glucose/dextrose solution can be used to prepare the solution for in vivo administration.

Ipilimumab (Yervoy) is an antibody inhibitor that blocks the inhibitory receptor cytotoxic T-lymphocyte antigen-4 (CTLA-4) on T cells, with immune-activating properties. Used for the treatment of unresectable or metastatic melanoma, this antibody exhibits antitumor activity.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent inhibitor of both mTOR (IC50: 38 nM) and PI3K, including PI3Kα (IC50: 6.6 nM), PI3Kγ (IC50: 6.6 nM), and PI3Kδ (IC50: 0.8 nM).

Tamarixetin (4'-O-Methyl Quercetin) is a natural flavonoid derivative of quercetin exhibiting multi-target biological activities including anti-inflammatory, antioxidant, antitumor, neuroprotective, and cardiovascular protective effects. Tamarixetin exerts its biological activity through multiple mechanisms such as direct radical scavenging, signaling pathway regulation, enzyme inhibition, and receptor binding.

OSMI-4 is a low nanomolar O-GlcNAc transferase (OGT) inhibitor (EC50 of 3 μM in cells) that can be used to study OGT inhibition in different human cell lines.

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

Vorinostat (SAHA) is a pan-histone deacetylase (HDAC) inhibitor (IC50=10 nM) with inhibitory activity against HDAC1/2/3/6/7/11. Vorinostat has antitumor activity, induces cell differentiation, blocks the cell cycle and induces apoptosis.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

Alpelisib (BYL-719) is a PI3Kα inhibitor (IC50=5 nM) with selective, potent, and oral activity, inhibiting PI3Kβ/γ/δ with low activity (IC50=250/290/1200 nM). Alpelisib demonstrates antitumor activity and specifically targets PIK3CA mutant tumors.

PF-573228 is an ATP-competitive FAK inhibitor. In a cell-free assay, the IC50 of FAK is 4 nM.

Alisertib (MLN 8237) is a specific Aurora A inhibitor (IC50: 1.2 nM). The selectivity of Alisertib(MLN 8237) is >200-fold higher for Aurora A than Aurora B.

PD98059 is an MEK inhibitor that inhibits MEK1 and MEK2 (IC50=2/50 μM) and is non-ATP-competitive. PD98059 is also antagonistic as a ligand for AHR. PD98059 inhibits autophagy.

(E)-Daporinad (FK866) is a highly specific, non-competitive small molecule inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with potential anti-tumor and anti-angiogenic activities with an IC50 value of 0.09 nM.

JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases.

4-Octyl Itaconate, a cell-permeable derivative of Itaconate, is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 and inhibits phosphorylation of STING.

C188-9 (TTI-101) is an orally administered, highly selective STAT3 SH2 domain inhibitor with a Kd value of 4.7 nM. C188-9 induces apoptosis in AML cell lines and primary samples while inhibiting colony formation in primary AML cells. C188-9 is suitable for studies on tumors, inflammation, and immune evasion.

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1/2/4/6 (IC50=36/47/510/1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma.

BLU0588 is a small-molecule inhibitor and a PRKACA-targeted inhibitor (IC50 = 1 nM, Kd = 4 nM), featuring high selectivity, cell permeability, and oral activity, suitable for experimental research and therapeutic development in fibrolamellar hepatocellular carcinoma (FLC).

SCH772984 is an ERK inhibitor that inhibits ERK1 and ERK2 (IC50=4/1 nM) and is highly selective and ATP-competitive. SCH772984 exhibits antitumor activity against BRAF or RAS mutant cells.

RBN-3143 is a potent inhibitor of NAD+-competitive catalytic PARP14 (IC50= 4 nM), which inhibits ADP-ribosylation mediated by PARP14 and stabilizes PARP14 in cell lines, demonstrating research potential for lung inflammation.

Zavondemstat (QC8222) is an orally active, selective inhibitor of the histone lysine demethylase 4 (KDM4) family, with an IC₅₀ of ≤ 0.08 μM against human KDM4A–D and a K₊₀ of 0.52 μM against human KDM4C. Zavondemstat activates tumor suppressor genes, induces apoptosis, causes S-phase cell cycle arrest, and inhibits cancer cell proliferation. In in vivo studies, Zavondemstat inhibits tumor growth and induces tumor regression. Zavondemstat can be used in cancer research.

Cadonilimab (AK104) is a tetravalent PD-1/CTLA-4 bispecific humanised antibody that activates T cells by enhancing IL-2 and IFN-γ secretion while reducing pro-inflammatory cytokine secretion (e.g., IL-6, IL-8). It offers low toxicity and high affinity, making it suitable for metastatic cervical, gastric, hepatic, and pulmonary cancers, pancreatic cancer, and oesophageal squamous cell carcinoma.