sk1 — TargetMol Chemicals

Cat No.	Product Name	Synonyms	Targets
T12927	SK1-IN-1		S1P Receptor
	SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM).		S1P Receptor
T30485	SK1-I	BML 258,BML-258,BML258,BML-258 HCl
	BML-258 HCl was removed and discontinued.
T60798	SK1- I hydrochloride
	SK1-I hydrochloride (BML-258 hydrochloride) is a sphingosine analog that can enhance autophagy and has antitumor activity. SK1-I hydrochloride is an isozyme-specific competitive SPHK1 inhibitor (Ki = 10 μM) [1] [2].
T12256	NS8593 hydrochloride	NS8593 HCl	Potassium Channel
	NS8593 hydrochloride (NS8593 HCl) is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .		Potassium Channel
T6085	PF-543	Sphingosine Kinase 1 Inhibitor II,PF 543	Apoptosis , S1P Receptor , Autophagy , LPL Receptor
	PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.		Apoptosis , S1P Receptor , Autophagy , LPL Receptor
T8840	PF-543 hydrochloride	PF-543	Apoptosis , S1P Receptor , Autophagy , LPL Receptor
	PF-543 hydrochloride (PF-543) inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.		Apoptosis , S1P Receptor , Autophagy , LPL Receptor
T9697	ASK1-IN-1		ASK
	ASK1-IN-1 is an inhibitor of apoptosis signal-regulating kinase 1 which is a key mediator in the apoptotic and inflammatory cellular stress response with an IC50 of 21 nM in biochemica assays.		ASK
TQ0311	GSK163090		Dopamine Receptor , 5-HT Receptor
	GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3).		Dopamine Receptor , 5-HT Receptor
T6003	GSK1904529A	GSK 4529	Apoptosis , Raf , VEGFR , IGF-1R , Syk
	GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .		Apoptosis , Raf , VEGFR , IGF-1R , Syk
T3079	GSK1838705A		IGF-1R , JNK , S6 Kinase , ALK
	GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.		IGF-1R , JNK , S6 Kinase , ALK
T67857	ASK1-IN-4		ASK
	ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.		ASK
T5427	GSK1940029	SCD inhibitor 1	Dehydrogenase , Stearoyl-CoA Desaturase (SCD)
	GSK1940029 (SCD inhibitor 1) is a stearoyl-coa desaturase (SCD) inhibitor.		Dehydrogenase , Stearoyl-CoA Desaturase (SCD)
T2357	GSK1059615	GSK 1059615,GSK-1059615	Apoptosis , PI3K , mTOR
	GSK1059615 has been used in trials studying the treatment of Lymphoma, Solid Tumours, Endometrial Cancer, Solid Tumor Cancer, and Metastatic Breast Cancer.		Apoptosis , PI3K , mTOR
T6848	GSK1016790A	GSK101	Calcium Channel , TRP/TRPV Channel
	GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.		Calcium Channel , TRP/TRPV Channel
T9377	ASK1-IN-2		Apoptosis , ASK , MAPK
	ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can potentially be used as a therapeutic strategy for ulcerative colitis[1].		Apoptosis , ASK , MAPK
T24105	GSK121	GSK-121,GSK 121	PAD
	GSK121 is an inhibitor of selective PAD4.		PAD
T27453	GSK1733953A	DG70	Antibacterial
	GSK1733953A can be used as a small molecule Mycobacterium tuberculosis respiration inhibitor with an inhibitory effect on MenG activity and an IC50 value of 2.6 ± 0.6 μM.GSK1733953A is a selective biphenylbenzamide with ...		Antibacterial
T2079	GSK126	GSK2816126A,EZH2 inhibitor	Histone Methyltransferase
	GSK126 (GSK2816126A) is a excellently specific EZH2 methyltransferase inhibitor ( IC50=9.9 nM).		Histone Methyltransferase
T3171	GSK137647A	GSK 137647	GPR
	GSK137647A (GSK 137647) is a selective FFA4 agonist.		GPR
T2701	GSK1292263		GPR
	GSK1292263 is a GPR119 agonist and has been investigated for the treatment of DIABETES MELLITUS, TYPE 2.		GPR
T15424	GSK1379725A		Epigenetic Reader Domain
	GSK1379725A is a selective BPTF ligand (Kd: 2.8 uM). It also shows no binding activity for Brd4.		Epigenetic Reader Domain
TQ0066	GSK189254A	GSK189254	Histamine Receptor
	GSK189254A (GSK189254) is a potent and specific histamine H3 receptor antagonist (pKi values: 9.59-9.90 and 8.51-9.17 for human and rat H3).		Histamine Receptor
T3513	GSK180736A	GSK180736	ROCK , GRK , PKA
	GSK180736A is an effective and selective GRK2 inhibitor (IC50: 0.77 μM) and >100-fold selectivity over other GRKs. It is a weak inhibitor of PKA (IC50: 30 μM), but highly effective against ROCK1 (IC50: 100 nM).		ROCK , GRK , PKA
T37450	SSK1		p38 MAPK
	SSK1 is a compound that selectively kills senescent cells and is a precursor for β-galactosidase, which can reduce the inflammatory response of the body. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in...		p38 MAPK
T6021	GSK1324726A	I-BET726	Apoptosis , Epigenetic Reader Domain
	GSK1324726A (I-BET726) is a greatly specific inhibitor of BET family proteins for BRD2(IC50=41 nM), BRD3(IC50=31 nM), and BRD4 (IC50=22 nM).		Apoptosis , Epigenetic Reader Domain
T8861	GSK199		PAD
	GSK199 is a selective PAD4 inhibitor(IC50 of 200 nM in the absence of calcium).		PAD
T24104	GSK106	GSK-106,GSK 106
	GSK106 is a negative control used in binding and functional assays for PAD4 inhibitors.
T27447	GSK1104252A	GSK 1104252A,GSK-1104252A
	GSK1104252A is a potent and selective agonist of GPR119.
T25467	GSK1360707	GSK-1360707,GSK 1360707
	GSK1360707 is a selective triple reuptake inhibitor (TRI).
T70171	GSK1379767A
	GSK1379767A is a dual inhibitor of BPTF and Brd4.
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]...
T15426	GSK180		Hydroxylase
	GSK180 is a selective competitive inhibitor of kynurenine 3-monooxygenase (KMO; IC50: ~6 nM), an enzyme involved in tryptophan metabolism.		Hydroxylase
T71069	GSK1842799 HCl
	GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. Upon phosphorylation, GSK1842799 showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3. GSK1842799 demonstrated good oral bioa...
T64011	GSK1820795A
	GSK1820795A, a telmisartan analog, functions as a selective antagonist of hGPR132a, inhibiting the activation of yeast cells that express hGPR132a by N-acylamides [1]. Additionally, it acts as an angiotensin II antagonis...
T60252	HSK16149
	HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit with analgesic activity.
T34653	SK1071
	SK1071 is a novel migrastatin analogs, which demonstrated improved performance over migrastatin, with nanomolar IC50 values in chamber cell migration assays with tumor cells and human umbilical vein endothelial cells (HU...
T68912	GSK1030058A
	GSK1030058A is a novel inhibitor of polo-like kinase
T27451	GSK1614343	GSK-1614343,GSK 1614343
	GSK1614343 is an antagonist of ghrelin receptor.
T11477	GSK1059865		Others
	GSK1059865 is a potent antagonist of the orexin 1 receptor.		Others
T38626	GSK143
	GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addi...
T32001	GSK124576A	GSK-124576A,GSK 124576A
	GSK124576A is a bioactive chemical.
T38619	GSK1795091	CRX-601
	GSK1795091 (CRX-601) is a synthetic TLR4 agonist and immunologic stimulator with demonstrated antitumor activity. It serves as a vaccine adjuvant, enhancing both mucosal and systemic immunity to influenza virus vaccines.
T32004	GSK172981	GSK 172981,GSK-172981
	GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional e...
T71343	GSK1997132B
	GSK1997132B is a potent, metabolically stable and centrally penetrant PPARγ partial agonist.
T39874	GSK143 dihydrochloride
	GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The c...
T11479	GSK1521498		Opioid Receptor
	GSK1521498 is a selective antagonist of the μ-opioid receptor (MOR). It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs.		Opioid Receptor
T73141	GSK1790627
	GSK1790627, the N-deacetylated metabolite of Trametinib, represents an orally active MEK inhibitor that promotes autophagy and triggers apoptosis [1].
T15425	GSK1702934A		Others
	GSK1702934A is a selective TRPC3 agonist. It modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.		Others
T32005	GSK1842799	GSK 1842799
	GSK1842799 is a selective S1P1 receptor agonist with good oral bioavailability.
T11478L	GSK1521498 free base		Opioid Receptor
	GSK1521498 free base is a potent and selective antagonist of the μ-opioid receptor. GSK1521498 free base also has the potential for disorders of compulsive consumption of food, alcohol, and drugs.		Opioid Receptor

Compounds

SK1-IN-1

T12927

Synonym: BML 258,BML-258,BML258,BML-258 HCl

Target: Potassium Channel

PF-543

T6085

Synonym: Sphingosine Kinase 1 Inhibitor II,PF 543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

PF-543 hydrochloride

T8840

Synonym: PF-543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Target: Dopamine Receptor, 5-HT Receptor

GSK1904529A

T6003

Synonym: GSK 4529

Target: Apoptosis, Raf, VEGFR, IGF-1R, Syk

GSK1838705A

T3079

Synonym:

Target: IGF-1R, JNK, S6 Kinase, ALK

Synonym: SCD inhibitor 1

Target: Dehydrogenase, Stearoyl-CoA Desaturase (SCD)

GSK1059615

T2357

Synonym: GSK 1059615,GSK-1059615

Target: Apoptosis, PI3K, mTOR

GSK1016790A

T6848

Synonym: GSK101

Target: Calcium Channel, TRP/TRPV Channel

ASK1-IN-2

T9377

Synonym:

Target: Apoptosis, ASK, MAPK

GSK121

T24105

Synonym: GSK-121,GSK 121

Target: Antibacterial

GSK126

T2079

Synonym: GSK2816126A,EZH2 inhibitor

Target: Histone Methyltransferase

Target: Epigenetic Reader Domain

GSK189254A

TQ0066

Synonym: GSK189254

Target: Histamine Receptor

GSK180736A

T3513

Synonym: GSK180736

Target: ROCK, GRK, PKA

Target: Apoptosis, Epigenetic Reader Domain

Synonym: GSK-106,GSK 106

Target:

GSK1104252A

T27447

Synonym: GSK 1104252A,GSK-1104252A

Target:

GSK1360707

T25467

Synonym: GSK-1360707,GSK 1360707

Synonym: GSK-1614343,GSK 1614343

Synonym: GSK-124576A,GSK 124576A

Synonym: GSK 172981,GSK-172981

GSK143 dihydrochloride

Target: Opioid Receptor

Target: Opioid Receptor

Cat No.	Product Name	Species	Expression System
TMPY-01635	PCSK1 Protein, Human, Recombinant (His)	Human	HEK293
	Neuroendocrine convertase 1, also known as Prohormone convertase 1, Proprotein convertase 1, PCSK1 and NEC1, is an enzyme which belongs to the peptidase S8 family and Furin subfamily. PCSK1 is an enzyme that performs the...

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Compounds

Recombinant Proteins

Compounds

Recombinant Proteins