acute

Revumenib (SNDX-5613) is a potent and selective oral inhibitor of menin-KMT2A interaction with Ki of 0.149 nM and IC50 between 10 and 20 nM, which can be used in the study of acute leukemia with MLL gene rearrangement.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Nrf2-IN-1 is an nuclear factor-erythroid 2-related factor 2 (Nrf2) inhibitor. Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).

GS-6201 (CVT-6883) is a selective antagonist of the adenosine A2B receptor, demonstrating high affinity and selectivity with a Ki of 22 nM for human adenosine A2B receptors.

Loteprednol etabonate (Lotemax) is an ophthalmic analog of the corticosteroid prednisolone with anti-inflammatory activity.

Moxifloxacin hydrochloride (BAY12-8039 HCl) is a fourth generation fluoroquinolone with expanded activity against gram-positive bacteria as well as atypical pathogens. Moxifloxacin has been linked to mild ALT elevations during therapy and to rare instances of idiosyncratic acute liver injury with symptoms and jaundice.

Pivanex (Pivalyloxymethyl butyrate) is an orally active HDAC inhibitor and an antimetastatic and antiangiogenic agent. Pivanex downregulates the Bcr-Abl protein and enhances apoptosis.

Kinetin (N6-Furfuryladenine), a type of cytokinin, has plant growth regulation effects.

Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM.

RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

SR33805 is a potent antagonist of Ca2+ channel(EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively)

Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH (Human Dihydroorotate Dehydrogenase) with antitumor activity, showing potential as a first-in-class candidate in AML [Acute Myeloid Leukemia].

BRD0705 is a potent, orally active GSK3α inhibitor with high selectivity (IC50: 66 nM; Kd: 4.8 μM), demonstrating an 8-fold higher selectivity for GSK3α compared to GSK3β (IC50: 515 nM).

TL02-59 is a selective inhibitor of Fgr in Src-family kinase (IC50 = 0.03 nM). TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia cell growth.

UC-514321 directly targets STAT3/5 and represses TET1 expression. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

CDKI-73 is a potent CDK9 inhibitor (Ki: 4 nM). It shows selective toxicity to CLL cells(LD50=80 nM) versus normal B cell and normal CD34+ cell(LD50>20 uM).The inhibition of CDK9 induces apoptosis and potentiates the effect of cisplatin.

Tandutinib (CT53518) (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.

5-BDBD is a potent and selective P2X4 receptor antagonist. 5-BDBD inhibits rP2X4R-mediated currents with an IC50 of 0.75 μM. 5-BDBD completely blocked the basal and acute hyperalgesia induced by NTG.

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants.

Plantamajoside (Y0160) has anti-hepatotoxic, anti-inflammatory, antinociceptive activities, improving sexual function and antioxidant activity.

Terevalefim (ANG-3777) is an hepatocyte growth factor (HGF) mimetic. Terevalefim selectively activates the c-Met receptor.

T.cruzi-IN-1 (MDK1088) is a Trypanosoma cruzi inhibitor.

Omadacycline (Amadacycline), a new tetracycline antibiotic, can inhibit the 30s subunit of bacterial ribosome.