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.

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.

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.

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.

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).

Daratumumab is a human monoclonal antibody that targets CD38 a cell surface protein that is overexpressed on multiple myeloma MM) cells.

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.

Magrolimab (Hu5F9-G4) is a humanized anti-CD47 IgG4 monoclonal antibody that exhibits antitumor activity by blocking CD47 and binding primarily to the N-terminal pyroglutamate of CD47. It can be used in combination with other compounds for the treatment of recurrent myeloma.

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.

Mezigdomide (CC-92480) is a potent, novel, selective and active cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue. Mezigdomide has anti-myeloma activity. [1]

(S)-Thalidomide ((S)-(-)-Thalidomide) is the S-isomer of Thalidomide with immunomodulatory, anti-inflammatory, anticancer, anti-angiogenic, and pro-apoptotic activities, used in studying leprosy erythema nodosum and myeloma.

Stilbamidine (Ba 2652) has antifungal and anticancer activity and can be used to study multiple myeloma and bladder migratory cell carcinoma.

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).

CPS-11 (N-(Hydroxymethyl)thalidomide) is a Thalidomide analogue with significant antitumor activity, exhibiting a broader and more potent effect on the MM (multiple myeloma) cell line.

Apomine (SR-9223i), an inhibitor of HMG-CoA-reductase, promotes apoptosis of myeloma cells in vitro and has been implicated in the regulation of myeloma in vivo. Apomine accelerates the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase and stimulates low-density lipoprotein receptor activity. Apomine enhances the antitumor effect of lovastatin on myeloma cells by downregulating 3-hydroxy-3-methylglutaryl-CoA reductase.

ProTAME is an inhibitor of APC/CFzr and APC/CCdc20. Combinations of proTAME with topoisomerase inhibitors, doxorubicin and etoposide, significantly increase cell death in primary cells and Multiple Myeloma (MM) cell lines, particularly if TOPIIα levels are first increased through pre-treatment with ProTAME.This compound is unstable in powder form and other related salt forms are recommended.

rac-CCT-250863 HCl is a selective and reversible inhibitor of NEK 2. rac-CCT-250863 HCl induces cell cycle arrest and has good anti-proliferative activity against cancer cells. rac-CCT-250863 HCl can be used in combination with Pomalidomide to induce apoptosis and can be used in combined anti-cancer studies.

Patamostat mesylate (E-3123) is a potent protease inhibitor with IC50 values of 39 nM for trypsin, 950 nM for plasmin, and 1.9 μM for thrombin. This compound demonstrates promising potential in suppressing the pathogenesis and development of acute pancreatitis.

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).

DT204 is an SCFSkp2 inhibitor that reduces the binding of Skp2 to Cullin-1 and Commd1. It can be used to study multiple myeloma.

Lem-14-1189, a LEM-14 derivative, is a potent NSD inhibitor of the nuclear receptor binding SET domain, and has inhibitory effects on NSD1, NSD2, and NSD3, with IC50 of 418 μM, 111 μM, and 60 μM, respectively. LEM-14-1189 has potential anticancer activity and can be used to study multiple myeloma (MM) and diseases of the blood system.

CC214-1 is an mTOR inhibitor with potential anticancer activity, inhibits protein translation, and induces autophagy. CC214-1 is an in vitro tool compound for exploring the biology of mTOR kinases and can be used to study myeloma.