malignancy

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

PU-H54 is a purine-based inhibitor of Grp94. It is a Grp94-selective resorcinol-based inhibitor isolated through probing of the exclusive binding region of S2 subpocket in Grp94.

Physcion 8-O-β-D-glucopyranoside (Physcion 8-O-beta-D-monoglucoside) has anti-inflammatory and anti-cancer activities. Physcion 8-O-β-D-glucopyranoside can be used in studies about common malignancy cancer.

Hypercalcemia Malignancy Factor (1-34), human is a polypeptide molecule with the sequence AVSEHQLLHDKGKSIQDLRRRFFLHHLIAEIHTA.

Suberoyl bis-hydroxamic acid (SBHA) is a Histone deacetylase (HDAC) inhibitor. HDAC is required for transcriptional modulation, cell cycle regulation and development. It is an enzyme that deacetylates lysine residues on the N-terminal of the core histones.

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.

Zoledronic Acid (ZOL 446) is a bisphosphonate. Zoledronic Acid (ZOL 446) is used to prevent skeletal fractures in patients with cancers such as multiple myeloma and prostate cancer. It can also be used to treat hypercalcemia of malignancy and can be helpful for treating pain from bone metastases. An annual dose of Zoledronate may also prevent recurring fractures in patients with a previous hip fracture. Zoledronic Acid (ZOL 446) is a single 5 mg infusion for the treatment of Paget's disease of bone. In 2007, the FDA also approved Reclast for the treatment of postmenopausal osteoporosis.

N1,N8-Diacetylspermidine is a polyamine found in human urine.N1,N8-Diacetylspermidine can be used as a marker for cancer and malignancy.

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.

Lonitoclax is an inhibitor of B-cell lymphoma 2 (Bcl-2). It demonstrates antitumor activity in B-cell and myeloid malignancy models comparable to Venetoclax. Lonitoclax holds potential for research in relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.

Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible inhibitor of kidney-type glutaminase (KGA). It binds to the glutamine binding site and forms a covalent bond with the cysteine residue at the active site. This compound selectively kills triple-negative breast cancer (TNBC) cells without being cytotoxic to control cell lines. KGA is an enzyme that regulates glutamine metabolism and is associated with tumor malignancy.

UNC7242 is an antagonist that binds to the Tudor domains of PHF1 and PHF19, with a Kd of 1.13 μM for PHF1 and 0.64 μM for PHF19. UNC7242 fails to displace full-length PHF1 or PHF19 from H3K36me3 nucleosomes or chromatin. UNC7242 is utilized in epigenetics research involving chromatin reader domain function, histone mark recognition, and polycomb-associated transcriptional regulation in malignancy-related biological systems.

FLT3/HDAC-IN-3 is a dual inhibitor targeting both FLT3 and HDAC. It shows potent inhibition of FLT3 (IC50 = 14 nM), HDAC1 (IC50 = 27 nM), HDAC6 (IC50 = 20 nM), and FLT3D853Y (IC50 = 55 nM), while exhibiting weak activity against HDAC8 and no activity against HDAC4. The compound is characterized by kinase selectivity, plasma stability, and stability in human liver microsomes. It demonstrates antiproliferative effects in various hematologic malignancy cell lines. In the Jeko-1 xenograft model, FLT3/HDAC-IN-3 exhibits inhibitory effects with no significant toxicity observed, making it useful for research in hematologic malignancies.

ND-2110, a selective interleukin-1 receptor-associated kinase 4 inhibitors, is used for the treatment of autoimmune disorders and lymphoid malignancy.

AZ5576, a potent and highly selective CDK9 inhibitor, can be used for research on Hematological Malignancy [1].

PI3Kδ-IN-11 is a potent and selective PI3Kδ inhibitor (IC50: 27.5 nM) that dose-dependently blocks PI3K/Akt pathway activity. PI3Kδ-IN-11 can be used in B- or T-cell-associated malignancy studies.

PI3Kδ/γ-IN-2 is a potent, orally bioavailable dual inhibitor of PI3Kδ (IC50: 1 nM) and PI3Kγ (IC50: 4.3 nM), with potential for use in anti-B-cell malignancy studies.

Zelavespib HCl is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. Zelavespib HCl shows antitumor activity in many preclinical models of malignancy. Zelavespib HCl has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.

A-1293201 is a potent and selective Bfl-1/A1 inhibitor (IC50 = 16 nM). It neutralizes anti-apoptotic signaling by binding the hydrophobic groove, used for hematological malignancy resistance research.

DS69910557, a potent, selective, and orally active antagonist of the human parathyroid hormone receptor 1 (hPTHR1), exhibits antagonistic activity with an IC50 value of 0.08 μM. It is useful in researching hyperparathyroidism, hypercalcemia of malignancy, and osteoporosis.

SD-6 is an effective dual Jak2 and Aurora A kinase inhibitor. It inhibits tumor cell proliferation by blocking STAT3 phosphorylation and inducing mitotic arrest, used for hematological malignancy research.

Lacto-N-fucopentaose II (LNFP II), a sialyl-Lewis hapten of the human Lewis blood group determinant, acts as a monosialo-ganglioside/glycolipid and sialyl derivative, CA 19-9, and is recognized as a molecular tumor marker (TM) for biliopancreatic malignancy [1].

SOR-C13 TFA, a truncated carboxy-terminal peptide, serves as a potent TRPV6 antagonist, demonstrating high affinity with an IC 50 value of 14 nM. TRPV6, a non-voltage-gated calcium channel linked to malignancy and poor prognosis in breast cancer, is effectively targeted by SOR-C13 TFA, indicating its anticancer activity [1].

Human PTHrP-(1-36) is a secreted parathyroid hormone-related protein with anticalciuric effects, promoting beta cell function and proliferation, and is used in research on humoral hypercalcemia of malignancy (HHM) and hyperparathyroidism [1] [3].