myeloma

Talmapimod (SCIO-469) is a selective, orally active, ATP-competitive p38α inhibitor with IC50 values of 9 nM for p38α and 90 nM for p38β. Talmapimod exhibits at least 2000-fold selectivity over a panel of 20 kinases, including other MAPKs.

MST-312 (Telomerase Inhibitor IX) is a derivative of green tea epigallocatechin gallate (EGCG). MST-312 is a telomerase inhibitor. MST-312 has research value in cancer, such as multiple myeloma (MM).

Lenalidomide (CC-5013) is an immunomodulator with oral activity. Lenalidomide is a ligand for the ubiquitin E3 ligase cereblon (CRBN), which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase, and is commonly used in the synthesis of PROTAC products.

Plerixafor (AMD-3329), a chemokine receptor antagonist, blocks the binding of stromal cell-derived factor (SDF-1alpha) to the cellular receptor CXCR4.

DCZ0415 induces antimyeloma activity in vitro, in vivo and in primary cells of drug-resistant myeloma patients. DCZ0415 is a potent TRIP13 inhibitor that can impair the repair of non-homologous end junctions and inhibit NF-κB activity.

BMS-P5 is a specific and orally active Peptidylarginine Deiminase 4 (PAD4) inhibitor.

BMS-P5 free base is a specific and orally active peptidylarginine deiminase 4 (PAD4) inhibitor that blocks the formation of Neutrophil Extracellular Traps and delays the progression of multiple myeloma. Administration of BMS-P5 to multiple myeloma-bearing mice delays symptom onset and disease progression. Targeting PAD4 may be beneficial for treating multiple myeloma.

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.

Lenalidomide hemihydrate is a derivative of Thalidomide, an orally active immunomodulator that acts as a molecular gel. It is a ligand for the ubiquitin E3 ligase cereblon, which selectively ubiquitinates and degrades two lymphoid transcription factors, IKZF1 and IKZF3, via the CRBN-CRL4 ubiquitin ligase.

OTS514 (OTS514 Hydrochloride) is a potent TOPK inhibitor. OTS514 exhibits a growth-suppressive effect on small cell lung cancer. OTS514 effectively suppressed the growth of SCLC cell lines (IC50: 0.4 ~ 42.6 nM). Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity. OTS514 treatment reduced CD90-positive SCLC cells and showed a higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.

Nelfinavir Mesylate (Viracept) is an effective HIV protease inhibitor (Ki: 2 nM).

NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor ( IC50=11 nM).

CCF642 (AC1LYELL) is a novel PDI-inhibiting compound with antimyeloma activity.

Nelfinavir (AG1341) is an antiretroviral drug used in the treatment of the human immunodeficiency virus (HIV) (Ki=2 nM). Nelfinavir is a broad-spectrum, anticancer agent.

Iberdomide (CC-220) is a modulator of cereblon( IC50 value of 60 nM in a competitive TR-FRET assay).

SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities

dCBP-1 is a chemical degrader of p300/CBP. dCBP-1 hijacks the E3 ubiquitin ligase CRBN for selective degradation of p300/CBP. Degradation of p300/CBP by dCBP-1 leads to effective multiple myeloma cell killing.

GSK3685032 is a non-covalent and selective DNMT1 inhibitor(IC50 = 36 nM). The inhibitory effect is time-independent and reversible. GSK3685032 induces loss of DNA methylation and transcriptional activation and inhibits cancer cell growth.

CDK9-IN-2 is a specific CDK9 inhibitor with an IC50 of 5 nM in the A2058 skin cell line (72 hours) and 7 nM in the H929 multiple myeloma cell line (72 hours).

(E/Z)-Zotiraciclib ((E/Z)-TG02) effectively inhibits CDK2, JAK2, and FLT3 with IC50s of 13 nM, 73 nM, and 56 nM, respectively.

PTC-209 is a potent and selective BMI-1 inhibitor.

ACY-241, also known as Citarinostat (ACY241), is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis.

CASIN (Pirl1-related Compound 2) is a specific inhibitor of GTPase Cdc42 (IC50: 2 uM).