pt 1

PT-1 is an AMPKα1 activator that dose-dependently activates AMPK α1394, α1335, and α2398 and enhances AMPK phosphorylation.

IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.

Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM). Etomoxir inhibits fatty acid oxidation by inhibiting CPT-1a, inhibits palmitate oxidation, has an inhibitory effect on adenine nucleotide translocase, and can inhibit macrophage polarization by disrupting CoA homeostasis.

Lunresertib (RP-6306) is a potent, selective, and orally active PKMYT1 inhibitor with an IC50 of 14 nM. Lunresertib (RP-6306) inhibits the growth of CCNE1-amplified tumor cells in several preclinical xenograft models.

McN3716 is a carnitine palmitoyltransferase I (CPT-1) inhibitor used for researching metabolic diseases.

Irinotecan hydrochloride trihydrate (CPT-11 HCl Trihydrate) keeps DNA from unwinding by inhibiting topoisomerase 1.

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Irinotecan (CPT-11), a derivative of camptothecin, is an inhibitor of DNA topoisomerase I (Topo I). Irinotecan has antitumor activity by preventing DNA strand reattachment through binding to the Topo I complex, resulting in double-stranded DNA breaks and cell death.

PT-179 is a novel IMiD derivative, a molecular gel.

Valylvaline acetate is a dipeptide and a PEPT1 agonist with an EC50 of 0.07mM.

TJ191 is a selective anti-cancer agent, targeting low TβRIII-expressing malignant T-cell leukemia/lymphoma cells.

PT-129 is a PROTAC degrader targeting the NTF2 domain of G3BP1/2, capable of inhibiting and degrading stress granules in stressed cells, disrupting ATF4 trafficking, and suppressing fibroblast-mediated cancer cell proliferation.

CU-CPT17e is a potent agonist of TLR(TLR3, TLR8, and TLR9).

Nosantine racemate, the racemic form of Nosantine, acts as an IL-2 inducer or enhances IL-2 induction by phytohemagglutinin (PHA).

Perhexiline maleate is an orally active inhibitor of CPT1 and CPT2, reducing fatty acid metabolism, with IC50 values of 77 μM and 148 μM against rat heart and liver CPT1, respectively.

Teglicar is a selective and reversible inhibitor of the liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1).

AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM). However, it has no effect on CCR5-using (R5) viruses. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC

PROTAC GSPT1 degrader-1 (Compound F) is a PROTAC-based degrader that effectively targets and degrades G1 to S phase transition protein 1 (GSPT1), achieving degradation rates of 95% at 1 μM and 86% at 0.1 μM. Additionally, this compound inhibits the viability of HL-60 cells with an IC50 of 9.2 nM.

PT109 is a multikinase inhibitor that targets JNK and other kinases, playing a crucial role in anti-inflammatory, antioxidative, neurogenic, and synaptogenic processes. Specifically, PT109 inhibits JNK isoforms with the following IC50 values: JNK1 at 0.143 μM, JNK2 at 0.831 μM, and JNK3 at 0.285 μM. It also inhibits SGK isoforms (SGK1: IC50=1.34 μM; SGK2: IC50=5.6 μM; SGK3: IC50=26.4 μM) and ROCK2 (IC50=34 μM). Additionally, PT109 reprograms polymorphic glioblastoma multiforme (GBM) into oligodendroglia via the PTBP1/PKM1/2 pathway and alters the metabolic pattern of GBM to exhibit antiglioma activity.

7-Bromohept-1-yne is a PROTAC Linker that can be used to synthesize AK-1690, a STAT6 (Signal transducer and activator of transcription 6) PROTAC degradator.

Bremelanotide is a synthetic peptide analog of alpha-MSH and is an agonist at melanocortin receptors including the MC3R and MC4R.

GSPT1 degrader-3 (Pro-2) is a CRBN-based BRDPROTAC degrader with a DC50 value of 21.1 nM.

PROTACFLT3/GSPT1/IKZF1/3 degrader-1 is an FLT3 PROTAC degrader with DC50 = 1.2 nM. It functions as a molecular glue to degrade its brain substrates and exhibits antiproliferative activity against resistant acute myeloid leukemia (AML) cells, showing potential applications in AML research.

GSPT1 degrader-7 (Example 43) is a molecular glue degrader targeting GSPT1 with an EC50 of 0.2 nM in DF15 multiple myeloma cells. It is applicable for cancer research.