53 Results for "

relatively selective

" in MedChemExpress (MCE) Product Catalog:
Products (53)

53 Results for "relatively selective" in MCE Product Catalog:

41
41 Publications Verification
Cat. No.: HY-10514
CAS No.: 702675-74-9
Purity:  99.84%
Target:  

PDK-1 IKK Autophagy

Research Areas:  

Cancer

BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy .
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13
13 Cited Publications
Cat. No.: HY-N2333
CAS No.: 57444-62-9
Synonyms: (+)-Resiniferatoxin
Resiniferatoxin ((+)-Resiniferatoxin), is a selective agonist of transient receptor potential vanilloid 1 (TRPV1) receptor agonist. Resiniferatoxin can be isolated from the Euphorbia resinifera plant. Resiniferatoxin eliminates TRPV1+ primary sensory afferents and blunt cardiac sympathetic afferent reflex for a relatively long period .
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10
10 Cited Publications
Cat. No.: HY-112780
CAS No.: 1394011-91-6
Purity:  99.92%
Target:  

MDM-2/p53 Apoptosis

Research Areas:  

Cancer

UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
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5
5 Cited Publications
Cat. No.: HY-15746
CAS No.: 49745-95-1
Purity:  99.60%
Dobutamine hydrochloride is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine hydrochloride is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine hydrochloride can increase cardiac output and correct hypoperfusion .
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5
5 Cited Publications
Cat. No.: HY-101836
CAS No.: 65836-72-8
Purity:  98.76%
Target:  

E1/E2/E3 Enzyme

Research Areas:  

Cancer

DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
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5
5 Cited Publications
Cat. No.: HY-15746A
CAS No.: 34368-04-2
Dobutamine is a synthetic catecholamine that acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors). Dobutamine is a selective β1-AR agonist, relatively weak activity at α1-AR and β2-AR. Dobutamine can increase cardiac output and correct hypoperfusion .
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3
3 Cited Publications
Cat. No.: HY-16950A
CAS No.: 68392-35-8
Synonyms: Afimoxifene; 4-OHT
(E/Z)-4-Hydroxytamoxifen (Afimoxifene) is a racemic compound of (Z)-4-Hydroxytamoxifen and (E)-4-Hydroxytamoxifen isomers. (E/Z)-4-Hydroxytamoxifen is a selective estrogen receptor modulator with mixed estrogenic and antiestrogenic activity, which is also an active metabolite of Tamoxifen (HY-13757A). (E/Z)-4-Hydroxytamoxifen is an agonist of the G protein-coupled estrogen receptor (GPER) with relatively low affinity (100-1000 nM). (E/Z)-4-Hydroxytamoxifen is promising for research of cyclical mastalgia, such as breast pain, tenderness, and nodularity .
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3
3 Cited Publications
Cat. No.: HY-10791
CAS No.: 87051-43-2
Purity:  99.68%
Synonyms: R 55667
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors .
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2
2 Cited Publications
Cat. No.: HY-16712
CAS No.: 1627503-67-6
Target:  

TGF-β Receptor

Research Areas:  

Cancer

LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
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1
1 Cited Publications
Cat. No.: HY-16940
CAS No.: 474-73-7
Synonyms: 24S-OHC; 24S-HC; Cerebrosterol
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators .
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1
1 Cited Publications
Cat. No.: HY-W011266
CAS No.: 627518-40-5
Target:  

PDGFR

Research Areas:  

Cancer

JNJ-10198409 is a relatively selective, orally active, and ATP competitive PDGF-RTK (platelet-derived growth factor receptor tyrosine kinase) inhibitor (IC50=2 nM). It is a dual-mechanism, antiangiogenic, and tumor cell antiproliferative agent. JNJ-10198409 has good activity against PDGFR-β kinase (IC50=4.2 nM) and PDGFR-α kinase (IC50=45 nM) .
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1
1 Cited Publications
Cat. No.: HY-14200
CAS No.: 185517-74-2
Purity:  99.80%
Synonyms: TVP1022; S-PAI
Target:  

Monoamine Oxidase

Research Areas:  

Neurological Disease

(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Cat. No.: HY-163638
CAS No.: 3094209-54-5
BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research .
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Cat. No.: HY-109968
CAS No.: 1005402-19-6
Purity:  99.38%
Synonyms: CEP-26401
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
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Cat. No.: HY-149262
CAS No.: 2922550-28-3
Purity:  98.03%
Target:  

CDK DYRK Autophagy

Research Areas:  

Cancer

CLK1-IN-3 (compound 10ad) is a potent and selective Clk1 inhibitor, with an IC50 of 5 nM and over 300-fold selectivity for Dyrk1A. CLK1-IN-3 also shows a relatively potent inhibition against Clk2 and Clk4, with IC50 values of 42 and 108 nM, respectively. CLK1-IN-3 potently induces autophagy in vitro. CLK1-IN-3 can be used for acute liver injury (ALI) research .
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Cat. No.: HY-100024
CAS No.: 1817791-73-3
Purity:  99.01%
Target:  

Mps1

Research Areas:  

Cancer

NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer .
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Cat. No.: HY-116871
CAS No.: 1957202-71-9
Purity:  98.67%
Target:  

CDK

Research Areas:  

Cancer

YKL-1-116 is a selective and covalent inhibitor of Cdk7. YKL-1-116 does not target Cdk9, Cdk12, or Cdk13. YKL-1-116 is more potent than THZ1 (HY-80013) toward both Cdk7 WT and Cdk7 as, although Cdk7 as is relatively resistant to this compound as well .
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Cat. No.: HY-101311
CAS No.: 168560-79-0
Purity:  99.89%
Synonyms: AIDA
Target:  

mGluR

Research Areas:  

Inflammation/Immunology Cancer

UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis .
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Cat. No.: HY-174445
CAS No.: 3107801-96-4
Research Areas:  

Cancer

C199 is a PROTAC degrader targeting PRMT4 (DC50 = 106 nM). C199 shows high selectivity for PRMT4 over other protein arginile methyltransferases. C199 exhibits strong cell degradation ability. C199 induces apoptosis in MM cell lines. C199 efficiently clears PRMT4 protein via the VHL-proteasome pathway. C199 has a relatively long half-life and shows strong anti-multiple myeloma (MM) tumor activity .
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Cat. No.: HY-125313
CAS No.: 139896-80-3
PSB-1737 is a human-selective GPR17 agonist with an EC50 for human GPR17 of 270 nM, and its activity on murine GPR17 is relatively weak (EC50 > 10 μM). PSB-1737 shows no significant inhibition at the glycine binding site of NMDA receptors, and has no significant agonistic or antagonistic activity on P2Y receptor subtypes. PSB-1737 can be used in demyelinating diseases (such as multiple sclerosis) or inflammatory-related anemia .
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