molt-4

Nelarabine (GW 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

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

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).

Puromycin dihydrochloride (CL13900 dihydrochloride) is a cinnamamide adenosine antibiotic and an inhibitor of protein synthesis. Puromycin dihydrochloride inhibits protein synthesis by binding to RNA and has antitumor and antitrypanosomal activity.

Daunorubicin hydrochloride (Rubidomycin hydrochloride), an anthracycline aminoglycoside antineoplastic, inhibits DNA replication and repair and RNA and protein synthesis.

Panobinostat (NVP-LBH589) is a broad-spectrum HDAC inhibitor (IC50=5 nM) with oral activity and non-selectivity. Panobinostat has antitumor activity and induces apoptosis and autophagy.

Selinexor HCl (1393477-72-9 free base) is an oral selective XPO1 (XPO1/CRM1) inhibitor that induces cell cycle arrest and apoptosis in tumor cells by blocking the transport of tumor suppressor proteins from the nucleus to the cytoplasm, thereby promoting their accumulation within the nucleus. Selinexor has been studied for the treatment of malignant tumors such as multiple myeloma.

Octaethylene glycol monododecyl ether (C12E8) is a non-ionic surfactant and detergent, suitable for assisting LOX activity assays and membrane protein extraction.

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar concentrations without damaging PLK1, a secondary target of AZD 1775.ZNL 02-096 induces degradation of Wee1 and accumulation of DNA damage in MOLT-4 cells in vitro, In vitro in MOLT-4 cells, ZNL 02-096 induced Wee1 degradation, accumulation of DNA damage, cell cycle arrest in G2/M phase and apoptosis.ZNL 02-096 showed anti-proliferative effects in 300 cancer cell lines.

LRK-4189 is an orally active, selective PIP4K2C PROTAC degrader with a DC50 <500 nM in MOLT-4 cells. It induces endogenous apoptosis and activates the interferon signaling pathway, exhibiting antitumor activity against microsatellite stable (MSS) colorectal cancer (CRC) cells.

Vercirnon (Traficet-EN) is a selective and potent antagonist of CCR9 (IC50: 10 nM). It is also used in the research of inflammatory bowel diseases.

BCL-XL-IN-3 (Compound 11) is an inhibitor of BCL-XL, with a Ki of less than 0.01 nM. It suppresses cell viability in both normal Molt-4 cells and digitonin-permeabilized Molt-4 cells, with EC50 values of 77.8 nM and 0.07 nM, respectively. BCL-XL-IN-3 can be utilized as an ADC toxin for synthesizing Clezutoclax.

LC-04-045 is a molecular glue degrader (MGD) of NEK7 (NIMA related kinase 7). This compound effectively degrades NEK7 in MOLT-4 cells, exhibiting a DC50 (half-maximal degradation concentration) of 7 nM and a Dmax (maximum degradation rate) of 90%. LC-04-045 displays high selectivity for NEK7 across the proteome and mediates NEK7 degradation via the ubiquitin-proteasome system (UPS), relying on a degradation motif that includes glycine 57 (G57) in NEK7. Additionally, LC-04-045 effectively inhibits the secretion of IL-1β and IL-18, with IC50 values of 33.03 nM and 32.99 nM, respectively. LC-04-045 is applicable for research in inflammatory diseases.

XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.

MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases, with IC50 values of 0.56 μM and 0.16 μM, respectively. This compound exhibits broad-spectrum anticancer activity, demonstrating potent effects against NCI-60 cancer cell lines, including SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM. By inhibiting Aurora A and MASTL kinases, MASTL/Aurora A-IN-1 induces G2/M phase cell cycle arrest, thereby impeding cancer cell proliferation. This compound is applicable for cancer research, particularly in the study of tumors with mitotic dysregulation.

Leuxinostat, an inhibitor of HDAC, exhibits an IC50 of 30 nM against hHDAC6. It suppresses the proliferation of THP1, K562, U937, and MEK1 cells, while also inducing apoptosis in leukemia cells NB4 and MOLT-4. Additionally, Leuxinostat inhibits the expansion of hematopoietic stem cells and demonstrates anti-leukemic activity in a zebrafish model.

PROTACERK5 degrader-1 (compound 2) is a bifunctional ERK5 PROTAC degrader. It induces the degradation of ERK5 in MOLT-4 cells via a VHL-mediated proteasome pathway. PROTACERK5 degrader-1 is useful for studying diseases or disorders characterized by abnormal ERK5 activity.

PZ671 is a potent PROTAC degrader targeting Bcl-xL, exhibiting an IC50 of 1.3 nM in MOLT-4 cells and a DC50 of 0.9 nM for Bcl-xL. It induces apoptosis in MOLT-4 cells and effectively inhibits tumor growth in MOLT-4 xenograft mice, while quickly restoring transiently reduced platelet counts. PZ671 is applicable in cancer research, including studies on small cell lung cancer.

BW-AQ-113 is a derivative of Anthraquinone that specifically degrades MDM2 and activates the p53 pathway. It exhibits IC50 values of 0.12 μM in Molt-4 cells and 0.2 μM in EU-1 cells. In p53-deficient K562 cells, p53-mutant T98G cells, and p53-inhibited HeLa cells, its IC50 values are 0.74, 5.2, and 2.1 μM, respectively. BW-AQ-113 induces apoptosis by downregulating the anti-apoptotic gene Bcl-2 and upregulating pro-apoptotic genes Bax and CASP3. Additionally, BW-AQ-113 can be utilized in research on hematologic malignancies with wild-type p53.

(Rac)-LRK-4189 is the racemate of LRK-4189. LRK-4189 (Compound 603) is an orally active, selective PIP4K2C PROTAC degrader with a DC50 of less than 500 nM in MOLT-4 cells. It possesses antitumor properties, inducing intrinsic cell death and activating interferon signaling, which leads to immune-mediated tumor killing in immune-inert microsatellite stable (MSS) colorectal cancer (CRC) cells. LRK-4189 is applicable in researching cancers such as MSS colorectal cancer.

Selective Cdk4 degrader. Degrades Cdk4 in Molt-4 cells, with no effect on Cdk6 levels. Displays cereblon-dependent degradation. Jiang et al (2019) Development of dual and selective degraders of cyclin-dependent kinases 4 and 6. Angew.Chem.Int.Ed.Engl. 58 6321 PMID:30802347

CTA 056 is an interleukin-2 induced T cell kinase (ITK) inhibitor, inhibits the growth of MOLT-4 xenograft tumors in mice, induces apoptosis in Jurkat cells, and can be used in the study of autoimmune disorders and T cell malignancies.

C24 dihydro Ceramide is a sphingolipid that has been found in the stratum corneum of human skin.[1] It is found in higher concentrations in female sebum compared to male sebum.[2] C24 dihydro Ceramide levels positively correlate with cytotoxicity in CCRF-CEM, MOLT-4, COG-LL-317h, and COG-LL-332h T cell acute lymphoblastic leukemia (ALL) cell lines.[4] Levels of C24 dihydro ceramide are increased by 149.49-fold in dihydroceramide desaturase 1 (DEGS1) knockdown UM-SCC-22A human head and neck squamous carcinoma cells in vitro.[4] C24 dihydro Ceramide levels are also increased in INS-1 β-cells incubated with glucose and palmitate.[5]