hematological

MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors.

R306465 (JNJ-16241199) is an orally active and selective class I histone deacetylase (HDAC 1) inhibitor with an IC50 of 3.3 nM. R306465 has a broad spectrum of antitumor activity, can induce histone 3 acetylation, and induce apoptosis, and can be used to study solid tumors and hematological malignancies.

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant properties that blocks alpha-adrenergic, histamine H1, and certain serotonin receptors; it may cause drowsiness and hematological issues.

Ibrutinib-MPEA is ibrutinib derivative. Ibrutinib is a covalent and irreversible BTK inhibitor that has been used to treat hematological malignancies.

Mevociclib (SY-1365) is a highly selective covalent inhibitor of CDK7, possessing therapeutic potential in both hematological and solid tumors.

T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025 can be used in studies about MYC-driven diseases.

Balapiravir (R1626, Ro 4588161) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479). IC50 Value: Target: HCV Balapiravir was discontinued for safety reasons in 28-36% of patients (m

Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

VLX 1500 is a potent deubiquitinating enzyme (DUBs) inhibitor designed to overcome resistance to traditional proteasome inhibitors. It triggers ER stress-mediated apoptosis by specifically blocking USP14/UCHL5 activity on the 19S regulatory particle, leading to a lethal accumulation of ubiquitinated proteins, widely used in drug target screening for relapsed hematological malignancies.

8-Chloroadenosine (NSC-354258) is a 5' AMP-activated protein kinase agonist potentially for the treatment of chronic lymphocytic leukemia. 8-chloroadenosine activity is associated with inhibition of the mTOR pathway.8-Chloroadenosine (NSC-354258) is a nucleoside analog; metabolized in vivo to 8-Chloro-ATP. Incorporates into RNA during transcription and inhibits RNA synthesis. Exhibits cytotoxicity in MM.1S, RPMI-8226, and U266 cancer cell lines; induces G2/M cell cycle arrest and mitotic catastrophe in A549 and H1299 cells. 8-Chloroadenosine (NSC-354258) has been shown to deplete ATP and inhibit tumor growth in hematological malignancies as well as in lung and breast cancer cell lines.

Enzomenib is a menin protein inhibitor that disrupts the interaction between menin and mixed lineage leukemia fusion proteins, thereby modulating transcriptional programs driven by MEN gene dysregulation and providing a targeted research tool for mechanistic studies and therapeutic exploration in hematological malignancies associated with menin-dependent oncogenic signaling.

FLT3/HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1/3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3/HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.

Vitamin A Propionate, an ester derivative of vitamin A, exhibits varying effects on growth, serum biochemistry, and hematological indices in foal nutrition studies depending on the dosage administered. Both excessively high and low doses lead to adverse impacts. These effects are correlated with the concentrations of vitamin A in the plasma, liver, and kidneys.

BMY-25551, a Mitomycin A analog, exhibits cytotoxicity 8 to 20 times greater than Mitomycin C against both murine and human tumor cell lines. It is applicable in research pertaining to cancer and hematological disorders.

MGD-28 is a potent, orally active Cullin-CRBN-dependent IKZF family protein degrader that dose-dependently degrades IKZF1 (Ikaros), IKZF2 (Helios), and IKZF3 (Aiolos) at nanomolar strengths.MGD-28 also degrades CK1α, and has shown antiproliferative activity against a variety of hematologic cancer cell lines showing antiproliferative activity in vitro and antitumor effects in in vivo assays, and is commonly used in multiple myeloma (MM) and hematological disorders.

AZD5991 is a potent and selective Mcl-1 inhibitor aimed at treating hematological cancers. As a well-designed macrocyclic compound, AZD5991 exhibits sub-nanomolar affinity for Mcl-1. It primarily inhibits the myeloid cell leukemia-1 protein (Mcl-1; Bcl2-L-3), showing potential pro-apoptotic and anti-tumor activity. AZD5991 binds to Mcl-1, preventing its interaction with certain pro-apoptotic proteins, leading to apoptosis in cells overexpressing Mcl-1.

AcBut-N-Ac-γ-Calicheamicin serves as a toxic molecule for ADCs, inducing cell cycle arrest and apoptosis (Apoptosis) by causing DNA double-strand breaks. Primarily utilized in the synthesis of antibody-drug conjugates (ADC), it holds promise for cancer research, particularly in studies related to acute lymphoblastic leukemia (ALL) and other hematological malignancies.

Bfl-1-IN-6 is a high-affinity Bfl-1/A1 inhibitor (IC50 = 19 nM). It neutralizes anti-apoptotic effects by binding to the hydrophobic groove of Bfl-1, sensitizing cancer cells to chemotherapy in hematological malignancy research.

FF2049 is a selective HDAC PROTAC degrader with a DC50 of 257 nM for HDAC1. It facilitates the ubiquitination and degradation of HDAC and promotes apoptosis (Apoptosis). FF2049 is applicable in research involving hematological and solid tumors.

PRMT5-IN-46 (compound 278) is a PRMT5 inhibitor (IC50 = 1–10 μM) applicable for studying proliferative diseases, metabolic disorders, and hematological conditions.

PROTAC HDAC6 degrader 2 (Compound 1) is an HDAC6 PROTAC degrader with an IC50 value of 0.643 μM. It facilitates the ubiquitination and degradation of HDAC6 and is applicable in research on hematological and solid cancers.

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.

GRK6-IN-4 is an inhibitor of G protein-coupled receptor kinase 6 (GRK6) with an IC50 value of 1.56 μM. GRK6-IN-4 is applicable for research related to hematological malignancies, inflammatory diseases, and autoimmune disorders.

GRK6-IN-5 is an inhibitor of the GRK6 polypeptide, with an IC50 of 4.48 μM. GRK6-IN-5 is utilized in research focused on hematological malignancies, inflammatory diseases, and autoimmune disorders.