Search Result

Search Results for " gi50 "

Targets

Compounds

Natural Products

Recombinant Proteins

Cat No.	Product Name	Synonyms	Targets
T10487	BCL6-IN-3		BCL , Others , DNA
	BCL6-IN-3 is a potent BCL6 inhibitor with GI50 of 70 nM in SU-DHL4 cells. BCL6-in-3 regulates cell activation, differentiation, DNA damage and apoptosis, and has antitumor activity.		BCL , Others , DNA
T15675	Tirbanibulin Mesylate	KX2-391 Mesylate,KX01 Mesylate	Microtubule Associated , Src
	Tirbanibulin Mesylate (KX01 Mesylate) is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).		Microtubule Associated , Src
T7411	Rbin-1	Ribozinoindole-1	ATPase , Phosphatase
	Rbin-1 (Ribozinoindole-1) is a potent,specific inhibitor of eukaryotic ribosome biogenesis.		ATPase , Phosphatase
T6691	TAI-1		Apoptosis , Microtubule Associated
	TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.		Apoptosis , Microtubule Associated
T41256	SP-96		Aurora Kinase
	SP-96 is a highly effective and selective inhibitor of Aurora B with an IC50 of 0.316 nM. SP-96 shows selective growth inhibition in NCI60 screening, including MDA-MD-468 (GI50=107 nM). SP-96 can be used in triple negati...		Aurora Kinase
T10325	ANI-7		Chk
	ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells and potently and selectively inhibits the growth of MCF-7 breast cancer cells (GI50: 0.56 μM).		Chk
T67873	USP8-IN-3		DUB
	USP8-IN-3 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with IC50 of 4.0 μM against USP8D. USP8-IN-3 inhibited the proliferation of GH3 and H1957 cells with GI50 values of 37.03 μM and 6.01 μM, res...		DUB
T21804	GW 610		Others
	GW 610 is an antitumor benzothiazole that shows growth-inhibitory activity against several cancer cell lines. In MCF-7 and MDA 468 human cancer cell lines, potent antiproliferative activity (growth inhibition (GI50) < 0....		Others
T5699	SSE15206		Apoptosis , Microtubule Associated
	SSE15206 is a microtubule polymerization inhibitor that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells.		Apoptosis , Microtubule Associated
T63136	DX3-213B		OXPHOS
	DX3-213B is a potent, orally active inhibitor of oxidative phosphorylation (OXPHOS) complex I with an IC50 of 3.6 nM. DX3-213B blocks ATP production (IC50: 11 nM) and inhibits the growth of MIA PaCa-2 cells (GI50: 11 nM)...		OXPHOS
T10898	Samuraciclib hydrochloride	ICEC0942 hydrochloride,CT7001 hydrochloride	Apoptosis , CDK
	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 h...		Apoptosis , CDK
T7057	Methylstat		Histone Demethylase , Others
	Methylstat is a methyl ester prodrug of a Jumonji C domain-containing histone demethylase (JMJD) inhibitor that has favorable cell permeability. The free acid of methylstat inhibits JMJD2A, JMJD2C, JMJD2E, PHF8, and JMJD...		Histone Demethylase , Others
T60146	USP8-IN-1		DUB
	USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].		DUB
T23552	YZ9		Glucokinase
	PFKFB3 inhibitor		Glucokinase
TQ0255	Olafertinib	CK-101,EGFR-IN-3,RX-518	EGFR
	Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC.		EGFR
T6345	Tirbanibulin	KX2-391,KX-01	Microtubule Associated , Src
	Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibit...		Microtubule Associated , Src
TQ0061	CHZ868		JAK
	CHZ868 is a type II JAK inhibitor with potential antitumor activity that reverses the persistence of type I JAK inhibitors and can be used to study leukemia.		JAK
T36816	S-trityl-L-Cysteine	STLC	Kinesin
	S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in ...		Kinesin
T15674	Tirbanibulin dihydrochloride	KX-01 (dihydrochloride),KX2-391 (dihydrochloride)	Src
	Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).		Src
T63542	SHR902275
	SHR902275 is a selective, potent, orally active RAF inhibitor capable of targeting RAS mutant cancers. SHR902275 acts on cRAF (IC50: 1.6 nM), bRAFwt (IC50: 10 nM), bRAFV600E (IC50: 5.7 nM). SHR902275 has cell growth inhi...
T10924	Cysteine protease inhibitor-2		Cysteine Protease
	Cysteine protease inhibitor 2 is a cysteine protease inhibitor. Cysteine protease inhibitor 2 inhibited DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.		Cysteine Protease
T63024	(Rac)-CFT7455
	(Rac)-CFT7455 is an Ikaros/Aiolos degradation agent that acts via the ubiquitin proteasome pathway and is able to act on NCIH929.1 cells (GI50: 0.05 nM). (Rac)-CFT7455 is a racemic isomer of CFT7455 and has anticancer ac...
T78977	Antitrypanosomal agent 12		Parasite
	Antitrypanosomal agent 12, a C20-phenylthiourea, exhibits trypanocidal and cytotoxic activities, demonstrating antitrypanosomal activity with GI50 values of 0.22 μM. It induces faster cell swelling in bloodstream-form tr...		Parasite
T63189	EGFR/BRAF-IN-1
	EGFR/BRAF-IN-1, a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent inhibitor of EGFR/BRAF, inhibiting BRAFV600E (IC50:45 nM) and cancer cell proliferation (GI50=35 nM), with good antioxidant effect.
T62869	OM-1700
	OM-1700 is a potent inhibitor of tankyrase, acting on tankyrase 1 (IC50: 127 nM) and tankyrase 2 (IC50: 14 nM). OM-1700 inhibits the growth of colon cancer cell lines and inhibits COLO 320DM cells (GI50: 650 nM).
T82931	Aurora A inhibitor 3		Aurora Kinase
	Aurora A Inhibitor 3 (Compound 5h) effectively inhibits Aurora-A kinase, exhibiting an IC50 of 0.78 μM, and demonstrates cytotoxicity against MCF-7 and MDA-MB-231 cell lines with GI50 values of 0.12 μM and 0.63 μM, respe...		Aurora Kinase
T63365	RAF-IN-1
	RAF-IN-1 is a potent inhibitor of b/cRAF, acting on cRAF (IC50: 3.8 nM), bRAFwt (IC50: 36 nM), bRAFV600E (IC50: 29.4 nM) and inhibiting A375 and H358 cell lines carrying the bRAFV600E mutation with a GI50 of 3.4 and 2.9 ...
T63996	EGFR-IN-50
	EGFR-IN-50 is a potent EGFR inhibitor targeting L858R resistance mutations, acting on TEL-EGFR-L858R-BaF3 and TEL-EGFR-T790M-L858R-BaF3 with GI50 values of 8 nM and 6.03 μM, respectively. EGFR-IN-50 exhibits anti-prolife...
T39889	Antitumor agent-23
	Antitumor agent-23 exhibits potent antitumoral activity, as demonstrated by its GI50 values of 38, 48, 5, 27, 80, and 28 nM against the lymphoma cell lines GRANTA-519, KARPAS-422, KARPAS-299, RAMOS, DAUDI, and RAJI respe...
T78978	Antitrypanosomal agent 13		Parasite
	Compound 4b (antitrypanosomal agent 13) is a potent antitrypanosomal with notable trypanocidal and cytotoxic activities, exhibiting GI50 values of 0.18 μM against T. brucei and 8.4 μM for HL-60 [1].		Parasite
T78759	VEGFR2-IN-4		VEGFR
	VEGFR2-IN-4 (compound 25) is a potent, selective inhibitor of the VEGFR2 kinase, exhibiting a GI50 of 0.7 nM and demonstrating anti-angiogenic effects. It is utilized in rheumatoid arthritis research [1].		VEGFR
T61576	Anticancer agent 83
	Anticancer Agent 83, a potent inhibitor of LOX IMVI cell growth, demonstrates anticancer efficacy with a GI50 value of 0.15 mM. It disrupts mitochondrial membrane potential and induces DNA damage, thereby promoting apopt...
T74300	MS143
	MS143, a potent AKT degrader (DC50=46 nM and GI50=0.8 µM in PC3 cells), effectively induces AKT degradation through the ubiquitin-proteasome system in both a concentration- and time-dependent manner, leading to the suppr...
T35650	Samuraciclib trihydrochloride
	Samuraciclib (CT7001) trihydrochloride is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib trihydrochloride displays 45-, 15-, 230- and 30-fold selectivity over C...
T78190	ERK1/2 inhibitor 9		ERK
	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-cy...		ERK
T79674	HDAC-IN-64		HDAC
	HDAC-IN-64 (Compound 13), an HDAC inhibitor, demonstrates potent inhibition of HDAC4/5/6/7/9 with IC50 values of 24, 45, 85, 31, and 37 nM, respectively. It exhibits anti-proliferative and anti-migration effects on prost...		HDAC
T61543	CLK1/4-IN-1
	CLK1/4-IN-1 (compound 31) is a highly potent and selective inhibitor of Clk1 and Clk4, with IC50 values of 9.7 nM and 6.6 nM, respectively. It effectively inhibits the growth of T24 cancer cells, with a GI50 value of 1.1...
T63650	Samuraciclib hydrochloride hydrate
	Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive, orally active inhibitor of CDK7 (IC50: 41 nM). Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines (GI50...
T36449	(S)-α-Methylbenzyl Ricinoleamide
	(S)-α-Methylbenzyl ricinoleamide is a fatty acid amide derived from ricinoleic acid and methyl benzylamine. It demonstrates potent growth inhibition of glioma (U251), breast (MCF-7), ovarian (NCI-ADR/RES and OVCAR-3), ki...
T37222	GLS1 Inhibitor
	GLS1 inhibitor is an inhibitor of glutaminase 1 (GLS1; IC50= 0.021 μM).1It inhibits the growth of NCI H1703 non-small cell lung cancer (NSCLC) cellsin vitro(GI50= 0.011 μM). GLS1 inhibitor (100 mg/kg) reduces tumor growt...
T79143	MS934		MEK
	MS934, a novel VHL-recruiting MEK 1/2 degrader, exhibits potent anti-proliferative effects on HT-29 cell growth, achieving a GI50 of 0.023 μM. It holds potential for researching various human cancers including melanoma, ...		MEK
T79708	SSE1806
	SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and antiproliferative properties. It demonstrates a GI50 for inhibiting canc...
T83009	Antitumor agent-107
	Antitumor agent-107 (compound 5h) is an anticancer agent that exhibits potent inhibitory activity against leukemia cell lines (GI 50 =0.32-1.34 μM), and demonstrates broad-spectrum antitumor effects across a range of oth...
T36458	CAY10701	CAY10701
	CAY10701 is a 7-deazahypoxanthine analog that prevents microtubule formation, blocking the proliferation of HeLa and MCF-7 cells (GI50s = 22 and 38 nM, respectively). It also inhibits the growth of several different colo...
T71287	CDKI-83
	CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determi...
T36099	Jacaric Acid
	Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants. Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid . Jacaric acid induces cell cycle arrest and a...
T72048	CDK8-IN-12		GSK-3 , CDK
	CDK8-IN-12 is a selective, potent and orally active inhibitor of CDK8 (Ki: 14 nM) and is an anti-cancer agent. CDK8-IN-12 inhibits GSK-3α, GSK-3β and PCK-θ with Ki of 13 nM, 4 nM and 109 nM respectively. CDK8-IN-12 showe...		GSK-3 , CDK
T68480	4SC-207
	4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell ...
T35428	β-Rubromycin
	β-Rubromycin is a bacterial metabolite originally isolated from Streptomyces that has diverse biological activities.1 It inhibits the growth of HMO2, KATO-III, and MCF-7 cells with GI50 values of 0.5, 0.84, and <0.1 μM, ...
T62763	VEGFR-2-IN-12
	VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent inhibitor of VEGFR-2 (IC50: 0.037 μM). VEGFR-2-IN-12 has anti-tumour effects.

Compounds

BCL6-IN-3

T10487

Synonym:

Target: BCL, Others, DNA

Tirbanibulin Mesylate

T15675

Synonym: KX2-391 Mesylate,KX01 Mesylate

Target: Microtubule Associated, Src

Rbin-1

T7411

Synonym: Ribozinoindole-1

Target: ATPase, Phosphatase

TAI-1

T6691

Synonym:

Target: Apoptosis, Microtubule Associated

SP-96

T41256

Synonym:

Target: Aurora Kinase

Target: Apoptosis, Microtubule Associated

Samuraciclib hydrochloride

T10898

Synonym: ICEC0942 hydrochloride,CT7001 hydrochloride

Target: Apoptosis, CDK

Methylstat

T7057

Synonym:

Target: Histone Demethylase, Others

Synonym: CK-101,EGFR-IN-3,RX-518

Target: EGFR

Tirbanibulin

T6345

Synonym: KX2-391,KX-01

Target: Microtubule Associated, Src

Tirbanibulin dihydrochloride

T15674

Synonym: KX-01 (dihydrochloride),KX2-391 (dihydrochloride)

Cysteine protease inhibitor-2

T10924

Synonym:

Target: Cysteine Protease

Antitrypanosomal agent 12

Target: Aurora Kinase

Antitrypanosomal agent 13

Samuraciclib trihydrochloride

Samuraciclib hydrochloride hydrate

T63650

Synonym:

Target:

(S)-α-Methylbenzyl Ricinoleamide

Cat No.	Product Name	Synonyms	Targets
TMA0958	Forsythoside F	Arenarioside	Xanthine Oxidase
	Forsythoside F (Arenarioside) is a natural product, and GI50 values of 10-16 microM against B16F10 cell.		Xanthine Oxidase
TN7041	(-)-Epipodophyllotoxin		Apoptosis
	(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vit...		Apoptosis
T21523	β-Tocotrienol	Beta-Tocotrienol	Caspase
	Beta-Tocotrienol to serve as a new anticancer agent for treating human lung and brain cancers. It inhibits the growth of both A549 (GI50=1.38±0.334μM) and U87MG (GI50=2.53±0.604μM) cells at rather low concentrations.		Caspase
TN3837	Desmethoxycentaureidin		Others
	Desmethoxycentaureidin shows high inhibitory activity against HeLa cell growth (GI50 9 microM).		Others
TN4355	Jolkinol A		Others
	Jolkinol A can inhibit both MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer) cell lines, with GI50 values ranging between 40.9 microM and 95.3 microM.		Others
T81769	Mollicellin I
	Mollicellin I (compound 1), a depsidone, exhibits minimal growth inhibitory activity against human breast cancer (Bre04), human lung (Lu04), and human neuroma (N04) cell lines, with GI50 values exceeding 10 μg/mL [1].
TN2493	1,4,5,6-Tetrahydroxy-7-prenylxanthone		Others
	1,4,5,6-Tetrahydroxy-7-prenylxanthone has anti-cancer activity, it shows moderate cytotoxicities against breast cancer (MDA-MB-435S) and lung adenocarcinoma (A549) cell lines; it also exhibits moderate activities with GI...		Others
T81201	Sartorypyrone B
	Sartorypyrone B, a 2β-acetoxyl analogue of chevalone C, is derived from the ethyl acetate extract of the culture of Neosartorya tsunodae (KUFC 9213), a fungus associated with marine sponges. This compound demonstrates po...
T72963	Anserinone B
	Anserinone B, a benzoquinone with antifungal and antibacterial properties, inhibits radial growth by 50% and 37% against S. fimicola and A. furfuraceus, respectively. Additionally, it demonstrates moderate cytotoxicity a...
T36749	Herboxidiene
	Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values rangin...

Natural Products

Forsythoside F

TMA0958

Synonym: Arenarioside

Target: Xanthine Oxidase

(-)-Epipodophyllotoxin

Synonym: Beta-Tocotrienol

Target: Caspase

Desmethoxycentaureidin

1,4,5,6-Tetrahydroxy-7-prenylxanthone

Recombinant Proteins

Species：

Expression System：

Tag：

Cat No.	Product Name	Species	Expression System
TMPY-04350	ICOS ligand Protein, Mouse, Recombinant (His)	Mouse	HEK293 Cells
	ICOS ligand Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 27.8 kDa and the accession number is Q544C7.
TMPY-00965	ICOS ligand Protein, Mouse, Recombinant (His & hFc)	Mouse	HEK293 Cells
	ICOS ligand Protein, Mouse, Recombinant (His & hFc) is expressed in HEK293 mammalian cells with His and hFc tag. The predicted molecular weight is 54.3 kDa and the accession number is Q544C7.

ICOS ligand Protein, Mouse, Recombinant (His)

TMPY-04350

Species: Mouse

Expression System: HEK293 Cells

ICOS ligand Protein, Mouse, Recombinant (His & hFc)

TMPY-00965

Species: Mouse

Expression System: HEK293 Cells