mt-1

MT1, a bivalent chemical probe targeting BET bromodomains, demonstrates an IC50 value of 0.789 nM for BRD4(1).

BMT-124110 is a selective AAK1 inhibitor (IC50: 0.9 nM) with antinociceptive activity. BMT-090605 inhibited BMP-2 induced protein kinase BIKE with IC50 of 17 nM. BMT-090605 inhibits cyclin G-associated kinase GAK with an IC50 of 99 nM.

BMT-124110 Formate is a selective AAK1 inhibitor (IC50: 0.9 nM) with anti-injury sensory activity.BMT-124110 Formate inhibits the BMP-2-inducible protein kinase BIKE with an IC50: 17 nM.BMT-124110 Formate inhibits the cell-cycle protein G-related BMT-124110 Formate inhibits the cell cycle protein G-associated kinase GAK with an IC50:99 nM.

BMT-145027 is a positive allosteric modulator of mGluR5 without inherent agonist activity (EC50 = 47 nM).

(Iso)-BMT-124110 Formate has an inhibitory effect on the protein serine/threonine kinase AAK, and is used in the treatment of Parkinson's disease, schizophrenia, neuropathic pain, and Alzheimer's disease.

BMT-108908 FA is a selective negative allosteric modulator of the NMDA receptor GluN2B subunit, with an IC50 of 4.2 nM in oocytes and antidepressant-like activity in mice, and can be used for treatment-resistant depression.

Mt KARI-IN-1 is a lead compound that demonstrates strong inhibitory activity towards Mycobacterium tuberculosis ketol-acid reductoisomerase (Mtb KARI), with a Ki value of 3.06 μM [1].

ZQMT-10 is an orally active TRPA1 inhibitor with a Kd of 1.04 μM, playing a significant role in cancer research.

BMT-108908 is a Negative Allosteric Modulator. It is selective for the NR2B Subtype of The NMDA Receptor Impair Cognition in Multiple Domains.

MT-134 is a SkMII-specific inhibitor with excellent muscle exposure.

ZLMT-12 (compound 35) is a tacrine derivative and a potent inhibitor of CDK2 (IC50: 0.011 μM) and CDK9 (IC50: 0.002 μM). ZLMT-12 weakly inhibits AChE (IC50: 19.023 μM) and BuChE (IC50: 2.768 μM). ZLMT-12 has anti-proliferative activity and low cytotoxicity. ZLMT-12 blocks the cell cycle in S-phase and G2/M-phase and induces apoptosis.

XMT-1519 conjugate-1 (compound 31) serves as a linker for the HER-2 monoclonal antibody XMT-1519, facilitating the synthesis of antibody-drug conjugates (ADCs) to enhance antitumor activity [1].

MT-1207 is a selective antagonist of adrenergic α1 and 5-HT2A receptors with oral activity. It exhibits IC50 values of <0.1 nM for α1A, 0.15 nM for α1B, 1.40 nM for α1D, and 0.27 nM for 5-HT2A. In the 2K2C rat model, MT-1207 effectively reduces blood pressure (BP) without impairing renal function. As a multitarget inhibitor, MT-1207 has potential for research in vasodilation.

ΧΜΤ-1519 conjugate-1 (compound 31) TFA is the linker for the HER-2 monoclonal antibody XMT-1519, used in the synthesis of antibody-drug conjugates (ADCs) to enhance anti-tumor activity.

Agomelatine (Valdoxan) is structurally closely related to melatonin. Agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2C (5-HT2C) receptors, tested in an animal model of depression.

Ramelteon (TAK-375) is a Melatonin Receptor Agonist. The mechanism of action of ramelteon is as a Melatonin Receptor Agonist.

Tasimelteon (BMS-214778) is a melatonin receptor agonist that is used for the treatment of non-24 hour sleep-wake disorder in blind individuals.

HIV-1 inhibitor-54 is a potent inhibitor of WT HIV-1 (strain IIIB) in MT-4 cells, demonstrating anti-HIV activity with an EC50 of 32 nM. [HIV-1 inhibitor-54 can be used to study viral infections.]

α-Vitamin E (Dexrabeprazole Sodium) is a naturally-occurring form of vitamin E, a fat-soluble vitamin with potent antioxidant properties.

1,2-Bis(2-iodoethoxy)ethane is a PEG-based PROTAC linker used in the synthesis of MT802 and SJF620, which are potent PROTAC BTK degraders with DC50s of 1 nM and 7.9 nM, respectively [1].

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values ​​of 8.16, 3.91, 1.14, and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m), and rat (r) MC1R, respectively. Dersimelagon exhibits good affinity for hMC1R and hMC4R, with Ki values ​​of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

IT1t dihydrochloride inhibits CXCL12/CXCR4 interaction with IC50 of 2.1 nM. IT1t dihydrochloride is an antagonist of CXCR4.

4'-Ethynyl-2'-deoxyadenosine (4'-E-dA), a nucleoside reverse transcriptase (RT) inhibitor, demonstrates potent activity against drug-resistant HIV variants, with an EC50 of 98 nM in MT-4 cells for anti-HIV-1 activity.

Mavorixafor trihydrochloride is a selective and orally available CXCR4 antagonist (IC50: 13 nM against CXCR4 125I-SDF binding) and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs (IC50s: 1 and 9 nM).