Cancer Targeted Therapy

5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a K_i of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia.

BRD6688 is a selective HDAC inhibitor with IC₅₀ values of 21 nM and 100 nM for HDAC1 and HDAC2, respectively. BRD6688 induces histone H4K12 and H3K9 acetylation. BRD6688 decreases CK2-induced HDAC2 phosphorylation. BRD6688 induces macrophage M1 to M2 polarization and renal cell proliferation. BRD6688 is used in research on neurodegenerative diseases, acute kidney injury, pain, and anxiety disorders.

Necrostatin-1 (Nec-1) (inactive control) is an inactive analog of Necrostatin-1 (HY-15760). Necrostatin-1 is a potent necroptosis inhibitor.

Enpp-1-IN-19 (compound 29f) is an orally active ENPP1 inhibitor that inhibits cGAMP hydrolysis by ENPP1 (IC₅₀=68 nM). Enpp-1-IN-19 increases anti-PD-L1 responses and inhibits tumor growth in CT26 syngeneic models. Enpp-1-IN-19 also enhances STING-mediated type I interferon responses, induces immune memory, and prevents tumor recurrence.

TMX-2039 is a pan-CDK inhibitor for both cell cycle CDKs (CDK1, CDK2, CDK4, CDK5 and CDK6) and transcriptional CDKs (CDK7 and CDK9), with IC₅₀s of 2.6, 1.0, 52.1, 0.5, 35.0, 32.5 and 25 nM, respectively. TMX-2039 acts as a Ligands for Target Protein for PROTACs.

c-Myc inhibitor 6 (compound A102) is a c-Myc inhibitor. c-Myc inhibitor 6 decreases cancer cell viability and degrades c-Myc protein. c-Myc inhibitor 6 can be used for the research of c-Myc imbalance, such as cancer, cardiovascular diseases, and viral infection.

DC-5163 is a potent glyceraldehyde-3-phosphate dehydrogenase (GAPDH) inhibitor with an IC₅₀ of 176.3 nM and a K_d of 3.192 μM. DC-5163 can inhibit glycolysis pathway partially. DC-5163 also selectively inhibits cancer cell proliferation and induces apoptosis.

3-(2-Pyridyldithio)propanoic Acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.

IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitor with an IC₅₀ of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.

Tigecycline tetramesylate (GAR-936 tetramesylate) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC₅₀ and MIC₉₀ are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.

L1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments.

PDS-0330 is a specific and potent Claudin-1 inhibitor. PDS-0330 interferes with claudin-1/Src association and inhibits colorectal cancer (CRC) progression and metastasis.

Fmoc-Asp-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Sulfo-LC-SPDP sodium is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Propargyl-PEG3-bromide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Propargyl-PEG3-bromide is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

3BP-4089 TFA is a highly efficient fibroblast activation protein (FAP) targeting peptide. 3BP-4089 TFA is often conjugated with radionuclides for tumor diagnosis and research.

CL 5343 (5-Amino-1,3,4-thiadiazole-2-sulfonamide) is a selective inhibitor of carbonic anhydrase B (HCA-B) and isoforms I, II, IV, and VII. CL 5343 has a K_i of 7.9 nM for hCA II. CL 5343 acts as a CA9 ligand to achieve targeted delivery of maytansine to the cell membrane of SKRC52 renal cancer cells. CL 5343 is useful in the development of therapeutics for diseases associated with CA overactivity, such as glaucoma, epilepsy, and cancer.

Solifenacin Succinate (YM905) is a novel muscarinic receptor antagonist with pK_is of 7.6, 6.9 and 8.0 for M₁, M₂ and M₃ receptors, respectively.

Fmoc-NH-ethyl-SS-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

PHGDH-IN-3 is an orally active phosphoglycerate dehydrogenase (PHGDH) inhibitor. PHGDH-IN-3 inhibits PHGDH with an IC₅₀ value of 2.8 μM. PHGDH-IN-3 can be used for the research of cancer.