Cancer Targeted Therapy

6-Alkyne-F-araNAD is an irreversible inhibitor of CD38. 6-Alkyne-F-araNAD helps other fluorescent probes (such as SR101−F-araNMN) to more clearly observe the localization of intracellular CD38.

PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC₅₀ of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC₅₀ of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.

hsa-miR-27a-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

hsa-miR-4506 antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

hsa-miR-5587-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.

hsa-miR-7109-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-3098-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

mmu-miR-6941-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

rno-miR-134-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.

Hydroxy-PEG10-acid (HO-PEG10-CH2CH2COOH) is a PEG-based non-cleavable ADC linker that can be used in the synthesis of Antibody-Drug Conjugates (ADCs).

TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA^G667C degradation (DC₅₀ = 24.69 nM; D_max > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1^G667C cells with an IC₅₀ value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research.

LC1236 is a thymidylate synthase (hTS) dimer dissociator with a target K_d of 7 μM and poor transmembrane permeability. LC1236 inhibits enzymatic activity by shifting the monomer-dimer equilibrium toward inactive monomers. LC1236 acts as a cytotoxic agent to inhibit cancer cell growth, and exerts synergistic cytotoxicity with electroporation via enhancing intracellular accumulation. LC1236 can be used in the research of cancers such as ovarian cancer and colorectal cancer.

Cryptolepine is an orally active multi-potent alkaloid with anti-cancer, anti-bacterial, anti-viral, anti-malarial, anti-inflammatory, anti-hyperglycemic, relieve pain and other properties. Cryptolepine acts as an inhibitor of c-Myc, mTOR, NF-κB, HIF-1, MAPK and an activator of AMPKα1/2. It intercalates into DNA, inhibits topoisomerase II (Top II), disrupts mitochondrial dynamics and induces apoptosis. Cryptolepine also exhibits anti-plasmodial and cholinesterase inhibitory activities. Cryptolepine can be used in research related to tumors (melanoma, hepatocellular carcinoma, mammary adenocarcinoma, etc.), malaria, inflammatory diseases and diabetes, particularly in studies focused on inhibiting tumor growth and anti-plasmodial infection.

Prolylserine, a dipeptide, is an inhibitor of melanogenesis production in Mel-Ab cells. Prolylserine decreases expression of microphthalmia-associated transcription factor (MITF) and tyrosinase, induces phorphosylation of ERK, but not cAMP response element binding protein (CREB).

Desmethyl-WEHI-345 analog is a protein kinase inhibitor extracted from patent WO2012003544A1, example 12. Desmethyl-WEHI-345 analog can be used for the research of colon cancer.

PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC₅₀s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC₅₀s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.

(S)-p-SCN-Bn-DOTA TFA is a bifunctional chelator (BFC), a macrocyclic DOTA (HY-W053583) derivative for tumor pretargeting. (S)-p-SCN-Bn-DOTA TFA can be used for the conjugation of peptides and radionuclides, such as as a linker for In-111 labeled radioimmunoconjugates (RICs) for single photon emission tomography (SPECT) and in vitro biodistribution studies.

(1s,4s)-C1-Piperidine-C1-cyclohexane-C1 is a PROTAC linker. (1s,4s)-C1-Piperidine-C1-cyclohexane-C1 can be used to synthesize PROTAC SMARCA2/4-degrader-33 (HY-162741).

MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer.

hsa-miR-3193 antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.