cdk9 inhibitor

CDK9 inhibitor HH1 (8019-9719) is an inhibitor of the human CDK2-cyclin A2 complex with an IC50 value of 2 μM.

Topoisomerase I Inhibitor 9 (compound 3d), a specific inhibitor of leishmanial topoisomerase IB, exhibits antileishmanial activity, demonstrating an IC50 value of 34.81μM against L. donovani promastigotes [1].

CDK9-IN-9 is a potent and selective CDK9 inhibitor (IC50: 1.8 nM) with anti-cancer activity. It inhibits CDK2 (IC50: 155 nM).

SIRT5 inhibitor 9 (compound 14), with an IC50 of 4.07 μM, is a competitive inhibitor of the sirtuin SIRT5, exhibiting potential anticancer properties [1].

Bromodomain inhibitor-9 is an inhibitor of Bromodomains that selectively inhibits the activity of BRD4-1 with a Kd value of 12 nM. Bromodomain inhibitor-9 can be used in studies of diseases related to systemic or lipid metabolism, tissue inflammation, fibrosis, or chronic autoimmune diseases.

MNK Inhibitor 9 is a potent, selective inhibitor of MNK1/2, demonstrating IC50 values of 0.003 µM for both MNK1 and MNK2. It exhibits good cell permeability, making it suitable for tumor-related research.

CypD inhibitor C-9 is a CypD inhibitor, it attenuates mitochondrial and cellular perturbation insulted by Aß and calcium stress.

Topoisomerase II inhibitor 9 is a Topo II inhibitor (IC50: 0.97 μM) and DNA embedding agent (IC50: 43.51 μM) that blocks the Hep G-2 cell cycle in the G2/M phase and induces apoptosis.

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. Among them, the RAS protein family is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 shows research potential for KRAS G12D-mediated cancer.

Caspase-9 Inhibitor III (Ac-LEHD-cmk), a caspase-9 inhibitor, exhibits protective effects against ischemia-reperfusion-induced myocardial injury.

PI3K/mTOR Inhibitor-9 (Compound 1) is a potent inhibitor of both mTOR and PI3K, acting on mTOR (IC50: 38 nM), PI3Kα (IC50: 6.6 nM), PI3Kγ (IC50: 6.6 nM) and PI3Kδ (IC50: 0.8 nM).

α-Synuclein inhibitor 9 (Compound 20C) is a molecule that targets and binds to cavities within mature α-synuclein fibrils, diminishing their β-sheet content. It effectively inhibits the aggregation of A53T α-synuclein and exhibits neuroprotective properties, enhancing brain functionality and alleviating motor impairments. This compound is utilized in research related to Parkinson's disease (PD). [1]

ATM Inhibitor-9 (Compd 7a) is a potent inhibitor of ATM kinase, exhibiting an IC50 value of 5 nM, and is utilized in cancer research [1].

Tuberculosis inhibitor 9 (compound 3d), a 3-methoxy-2-phenylimidazo[1,2-b]pyridazine derivative, exhibits potent activity against Mycobacterium tuberculosis and Mycobacterium marinum, with an MIC 90 of 0.64 μM for both organisms [1].

MMP-2/MMP-9-IN-1 is a potent, highly selective and orally bioavailable inhibitor of type IV collagenases (MMP-9 and MMP-2) with an IC50 of 0.24 and 0.3 1 μM for MMP-9 and MMP-2, respectively. activity, which can be used to study cancer.

Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B bipolar kinase inhibitor, acting on Aurora A (IC50: 0.093 μM), Aurora B (IC50: 0.09 μM). broad-spectrum anti-proliferative activity.

Mcl-1 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.

Chitin synthase inhibitor 9 is a chitin synthase (CHS) inhibitor that exhibits broad-spectrum antifungal activity and can be used in studies of fungal infections.

CDK-IN-9 (compound 24) is a potent inhibitor of CDK. CDK-IN-9 is also a molecular gel that induces interaction between CDK12 and DDB1 and is able to act on CDK2/E (IC50: 4 nM). CDK-IN-9 can be used to dephosphorylate retinoblastoma protein and RNA polymerase II, thereby inducing apoptosis.

MMP-9/MMP-13 Inhibitor I is a dual inhibitor of MMP-9 and MMP-13 with IC50 of both 0.9 nM. MMP-9/MMP-13 Inhibitor I is over 20 times more selective for MMP-9/MMP-13 than other MMPs.

FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM. It targets the ATP-binding pocket of FGFR1 and demonstrates anticancer activity [1].

c-Myc Inhibitor 9 (Compound 332) is an effective c-Myc inhibitor, exhibiting a logEC50 of ≥6, and demonstrating significant tumor growth inhibition in nude mouse models. This compound is utilized in cancer research.

Carbonic anhydrase inhibitor 9 is a potent inhibitor of carbonic anhydrase (CA) that acts on hCA II (Ki: 56.4 nM) and IX (Ki: 56.9 nM) and exhibits antiproliferative effects.

HIV-1 inhibitor-9 exhibits potent inhibition activity at low nanomolar concentrations against both the wild-type (WT) HIV-1 strain and multiple strains that have developed resistance to non-nucleoside reverse transcriptase inhibitors (NNRTIs).

ProMMP-9 inhibitor-3c is a potent and specific proMMP-9 inhibitor which disrupts f MMP-9 homodimerization and prevents association of proMMP-9 with both α4β1 integrin and CD44 and results in the dissociation of EGFR.

ERK1/2 Inhibitor 9 (Probe 1), a covalent antagonist of ERK1/2, exhibits sub-micromolar efficacy in cellular assays (A375 GI50=0.47 μM) and facilitates the reduction of phospho-ERK1/2 levels. When conjugated with trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine-tagged Thalidomide), it forms the corresponding ERK-CLIPTAC, promoting targeted ERK1/2 degradation [1].

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

HIV-1 integrase inhibitor 9 (compound 8a) is a potent inhibitor of HIV-1 RNase H (IC50: 12.3 μM) and has antiviral effects.

MMP-9 inhibitor I is an inhibitor of matrix metalloproteinase-9 (MMP-9) that is selective over MMP-1 and MMP-13 (IC50s = 5, 1,050, and 113 nM, respectively). It also decreases the activity of TNF-α converting enzyme (TACE) in a dose-dependent manner (IC50 = 0.54 μM). MMP-9 inhibitor I decreases TNF-α secretion stimulated by LPS in BV-2 microglial cells when used at concentrations of 50 and 100 μM.

ATX inhibitor 9 is a thickened heteroaryl derivative compound and a potent inhibitor of ATX. Among them Autotaxin (ATX), also known as ENPP2, is a secreted enzyme highly expressed mainly in lung cancer cells, bronchial epithelial cells and alveolar macrophages.ATX inhibitor 9 has research potential for cancer or fibrous degenerative diseases.

KRAS inhibitor-9 (DUN09716) is a potent KRAS inhibitor with Kd of 92 μM that blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSC-LC cells with KRAS mutation but not normal lung cells

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

Dinaciclib (SCH 727965) is a CDK inhibitor that selectively inhibits CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). Dinaciclib has potential antitumor activity and inhibits the incorporation of thoracic glycan (dThd) DNA.

SEL120-34A is a selective and ATP-competitive inhibitor of CDK8 with IC50s of 4.4 nM, 10.4 nM and 1070 nM for CDK8/CycC, CDK19/CycC and CDK9/cycT. SEL120-34A possesses antitumor activity.

PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively.

(S)-Enitociclib (VIP152) is a selective CDK9 inhibitor that induces complete regression of MYC+ lymphomas by inhibiting RNA polymerase II-mediated transcription of anti-apoptotic and pro-survival proteins.

(R)-Enitociclib, an enantiomer of BAY-1251152, is a CDK9 inhibitor with anticancer activity.

BUR1 is a selective BMP upregulator that acts by increasing the expression of Inhibitor of DNA binding 1 and inducing BMP2 and PTGS2 expression.

CDK9-IN-2 is a special CDK9 inhibitor and has an IC50 of 5 nM and 7 nM in A2058 skin cell line (72 hours) and H929 multiple myeloma cell line (72 hours), respectively.

CDK9-IN-8 is a highly potent and selective CDK9 inhibitor (IC50: 12 nM).

CDK9-IN-10 is a potent CDK9 inhibitor and the ligand for the PROTAC CDK9 degrader-2.

CDK9-IN-7 is a highly selective and orally active CDK9/cyclin T inhibitor (IC50: 11 nM), which exhibits more potent over other CDKs (CDK4/cyclinD: 148 nM; CDK6/cyclinD: 145 nM).

LDC000067 (LDC067) is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.

NVP-2 is an effective and selective ATP-competitive cyclin-dependent kinase 9 (CDK9) probe. NVP-2 induces cell apoptosis. NVP-2 inhibits CDK9/CycT activity (IC50: 0.514 nM). NVP-2 shows inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases (IC5

(±)-Enitociclib ((±)-BAY-1251152) is a racemic mixture of BAY-1251152. BAY-1251152 is highly selective inhibitor of PTEF/CDK9.

Bohemine is a cyclin-dependent kinase inhibitor.

BS-181 is a highly selective CDK7 inhibitor (IC50: 21 nM); >40-fold selective for CDK7 than CDK1/2/4/5/6/9.

AT7519 is a CDK1/2/4/6/9 inhibitor (IC50: 10-210 nM). It is less effective to CDK3 and little active to CDK7.

Samuraciclib hydrochloride (ICEC0942 hydrochloride) is a potent, selective, ATP competitive and oral active CDK7 inhibitor with IC50 of 41 nM. The selectivity of Samuraciclib hydrochloride is 45-, 15-, 230- and 30-fold higher than CDK1, CDK2 (IC50 is 578 nM), CDK5 and CDK9 respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 μM. Samuraciclib hydrochloride has anti-tumor effects.

FIT-039 is a selective and ATP-competitive, orally active inhibitor of CDK9( IC50 : 5.8 μM;CDK9/cyclin T1). FIT-039 inhibits replication of HSV-1 (IC50 of 0.69 μM), HSV-2, human adenovirus, and human CMV. FIT-039 is a promising antiviral agent for inhibiting drug-resistant HSVs and other DNA viruses.